☆ 4.8 Review

Small-molecule probes from bench to bedside: advancing molecular analysis of drug-target interactions toward precision medicine

CHEMICAL SOCIETY REVIEWS (2023)

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Article Biochemistry & Molecular Biology

A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo

Atsunori Kaneshige et al.

Summary: AK-2292 is a potent and selective small-molecule degrader of both STAT5A and STAT5B isoforms. It selectively inhibits STAT5 activity and induces degradation of STAT5A/B proteins without affecting other STAT proteins and numerous non-STAT proteins. AK-2292 effectively induces STAT5 depletion in both normal tissues and CML xenograft tissues, leading to tumor regression in CML xenograft mouse models. It is not only a powerful research tool to study STAT5 biology and therapeutic potential, but also a promising lead compound for STAT5-targeted therapy development.

NATURE CHEMICAL BIOLOGY (2023)

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Article Chemistry, Multidisciplinary

Revisiting PFA-mediated tissue fixation chemistry: FixEL enables trapping of small molecules in the brain to visualize their distribution changes

Hiroshi Nonaka et al.

Summary: Various small molecules have been used in medical diagnosis and disease treatment. However, evaluating the spatial distribution and kinetics of these molecules in complex tissues, such as the brain, has been challenging. This study introduces a new method called FixEL, which utilizes protein-MOI interactions and chemical cross-linking to trap and image exogenously administered molecules in complex tissues, providing valuable information on their distribution, binding selectivity, and diffusion/retention kinetics.

CHEM (2023)

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Article Engineering, Biomedical

Near-infrared fluorescence lifetime imaging of amyloid-β aggregates and tau fibrils through the intact skull of mice

Steven S. S. Hou et al.

Summary: A fluorophore with peak near-infrared excitation and emission wavelengths enables imaging of amyloid-beta and tau aggregates in mouse models of Alzheimer's disease through intact skull. This non-invasive method facilitates the study of disease progression and potentially aids in early diagnosis in humans.

NATURE BIOMEDICAL ENGINEERING (2023)

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Article Chemistry, Multidisciplinary

Targeted activation in localized protein environments via deep red photoredox catalysis

Nicholas Eng Soon Tay et al.

Summary: State-of-the-art photoactivation strategies in chemical biology provide control and visualization of biological processes. However, using high-energy light for sensitization can lead to background activation of probes. This study presents the development of targeted aryl azide activation via deep red-light photoredox catalysis and its application in photocatalysed proximity labelling.

NATURE CHEMISTRY (2023)

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Article Multidisciplinary Sciences

Tracking chromatin state changes using nanoscale photo-proximity labelling

Ciaran P. Seath et al.

Summary: Interactions between biomolecules are important for cellular processes and can be disrupted by mutations or external factors, leading to changes in cellular physiology, which can have disease or therapeutic effects. Studying these interactions and their response to stimuli is crucial for drug development, leading to improvements in human health.

NATURE (2023)

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Article Chemistry, Multidisciplinary

OregonFluor enables quantitative intracellular paired agent imaging to assess drug target availability in live cells and tissues

Lei G. Wang et al.

Summary: Non-destructive diffusion of fluorescent molecules across cell membranes is crucial for quantitative imaging in live cells and tissues. We have developed biologically compatible and cell-membrane-permeable fluorophores called OregonFluor (ORFluor), which allow for quantitative visualization of their intracellular distribution and protein target-specific binding using ratiometric imaging methodology. This provides a chemical toolkit for quantifying drug target availability in live cells and tissues.

NATURE CHEMISTRY (2023)

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Article Chemistry, Multidisciplinary

A fluorogenic-inhibitor-based probe for profiling and imaging of monoamine oxidase A in live human glioma cells and clinical tissues

Haixiao Fang et al.

Summary: The researchers reported HD1 as the first fluorogenic-inhibitor-based probe that can selectively label endogenous MAO-A from various mammalian cells and clinical tissues. The probe was designed based on N-propargyl tetrahydropyridine, a small MAO-A-specific fluorogenic and inhibitory war-head, so that the probe becomes fluorescent upon in situ enzymatic oxidation and covalent labeling of MAO-A. With excellent binding affinity and fluorogenic properties, HD1 offers a promising approach for imaging endogenous MAO-A activities and studying its drug interactions.

SCIENCE CHINA-CHEMISTRY (2023)

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Article Engineering, Biomedical

A hydrogel-based mechanical metamaterial for the interferometric profiling of extracellular vesicles in patient samples

Haitao Zhao et al.

Summary: Researchers have developed a hydrogel-based metamaterial that can molecularly profile extracellular vesicles in the ascites fluid of cancer patients. This mechanically responsive metamaterial can amplify shape and optical changes through antibody-mediated biorecognition, and its detection can be done using a smartphone camera.

NATURE BIOMEDICAL ENGINEERING (2023)

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Review Biochemistry & Molecular Biology

Epigenetic regulation in hematopoiesis and its implications in the targeted therapy of hematologic malignancies

Ailin Zhao et al.

Summary: Hematologic malignancies are common and incurable cancers that have been increasing in incidence. The epigenetic regulation, including DNA modifications, histone modifications, and noncoding RNA-mediated targeting, plays a vital role in hematologic oncogenesis. Abnormal methylation profiles and histone deacetylase expression are frequently found in leukemia and lymphoma. Hypomethylating agents and histone deacetylase inhibitors have shown effectiveness in treating certain hematologic malignancies. This review comprehensively discusses the role of epigenetic regulators in normal and oncogenic hematopoiesis and their implications in targeted treatment.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2023)

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Review Chemistry, Multidisciplinary

Activatable fluorescent probes for in situ imaging of enzymes

Xiaofeng Wu et al.

Summary: This article summarizes the methods for in situ imaging of enzymes using activatable fluorescent probes, and proposes that fluorescent probes with both activatable and in situ properties will facilitate high-resolution studies of enzymes in living systems.

CHEMICAL SOCIETY REVIEWS (2022)

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Article Chemistry, Multidisciplinary

Development of Photolenalidomide for Cellular Target Identification

Zhi Lin et al.

Summary: This study reports the development of photolenalidomide (pLen), a Len probe with a photoaffinity label and enrichment handle, designed for target identification by chemical proteomics. Using pLen, the known targets IKZF1 and CRBN were captured, and a new target, eIF3i, was identified. These data suggest the existence of a broader array of targets induced by ligands to CRBN, which can be identified using pLen in additional biological systems.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2022)

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Article Multidisciplinary Sciences

Low-dose metformin targets the lysosomal AMPK pathway through PEN2

Teng Ma et al.

Summary: The molecular target of the antidiabetic medicine metformin is identified as PEN2, and the PEN2-ATP6AP1 axis activates the AMPK pathway, providing therapeutic effects without substantial adverse effects.

NATURE (2022)

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Article Biochemical Research Methods

Engineered HaloTag variants for fluorescence lifetime multiplexing

Michelle S. Frei et al.

Summary: HaloTag variants offer unique brightness and fluorescence lifetimes compared to HaloTag7 when labeled with rhodamines, enabling multiplexed imaging and creating cell cycle indicators. These variants are powerful tools for fluorescence microscopy and can be used to generate fluorescence lifetime-based biosensors, with the brightest variant showing up to 40% higher brightness in live-cell imaging applications.

NATURE METHODS (2022)

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Article Multidisciplinary Sciences

The AUTOTAC chemical biology platform for targeted protein degradation via the autophagy-lysosome system

Chang Hoon Ji et al.

Summary: In this study, the authors develop a targeted protein degradation platform called AUTOTAC to degrade oncoproteins and neurodegeneration-associated proteins via the p62-dependent autophagy-lysosome system.

NATURE COMMUNICATIONS (2022)

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Review Medicine, Research & Experimental

An update of label-free protein target identification methods for natural active products

Zhao Cui et al.

Summary: This article reviews the current protein target identification methods for natural active products (NAPs), with a focus on the progress of label-free identification methods.

THERANOSTICS (2022)

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Article Radiology, Nuclear Medicine & Medical Imaging

Two experts and a newbie: [18F]PARPi vs [18F]FTT vs [18F]FPyPARP-a comparison of PARP imaging agents

Sophie Stotz et al.

Summary: The study introduced a novel radiotracer [F-18]FPyPARP with higher renal clearance and an easily translatable synthesis route for potential clinical application, aiming to address the issue of hepatobiliary clearance in [F-18]PARPi and [F-18]FTT for abdominal lesion detection. Comparative study in mice showed [F-18]FPyPARP had a partial shift from hepatobiliary to renal clearance, making it a potential alternative for PET imaging of PARP enzymes compared to [F-18]PARPi and [F-18]FTT.

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2022)

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Article Biochemistry & Molecular Biology

In situ identification of cellular in mammalian tissue

Zhengyuan Pang et al.

Summary: This study develops a clearing-assisted tissue click chemistry (CATCH) technique for optically imaging covalent drug targets in intact mammalian tissues. The researchers find that CATCH enables specific and robust imaging of target-bound drug molecules at subcellular resolution, and it can also identify the target cell types. By using inhibitors of endocannabinoid hydrolases and monoamine oxidases, the study not only reveals distinct anatomical distributions and predominant cell targets of different drug compounds in the mouse brain, but it also uncovers unexpected differences in drug engagement across and within brain regions, reflecting rare cell types and dose-dependent target shifts that cannot be accessed by conventional methods.

CELL (2022)

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Review Biochemistry & Molecular Biology

BET bromodomain inhibitors

Martin P. Schwalm et al.

Summary: Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins, which are important regulators of linage specific gene transcription. The development of potent and selective inhibitors has facilitated mechanistic studies in disease models and translation into clinical practice. Advances in pan-BET inhibitors have led to second generation inhibitors with improved selectivity, as well as highly potent bifunctional and dual inhibitors, expanding the toolbox for research on acetylation dependent transcription, BET-associated diseases, and epigenetic reader domains.

CURRENT OPINION IN CHEMICAL BIOLOGY (2022)

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Article Chemistry, Medicinal

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Yue Zhong et al.

Summary: Targeted protein degradation technology represents a new therapeutic modality in drug discovery. Researchers are exploring optimized protein degraders to overcome the limitations of classical PROTACs and achieve more precise protein degradation.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

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Review Biochemistry & Molecular Biology

Radiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade

George Crisan et al.

Summary: Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) are imaging techniques that use radioactive tracers. PET is mainly used for measuring metabolic processes, blood flow, and chemical composition, while SPECT is used for diagnosing conditions such as strokes, bone diseases, and infections. This article provides a systematic review of the scientific literature on PET/SPECT radiotracers and gives an overview of the research conducted in the past decade, with a focus on novel radiopharmaceuticals for medical imaging.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

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Article Radiology, Nuclear Medicine & Medical Imaging

High-resolution and high-sensitivity PET for quantitative molecular imaging of the monoaminergic nuclei: A GATE simulation study

Zipai Wang et al.

Summary: This article introduces a new high-resolution and high-sensitivity brain-dedicated PET scanner using depth-encoding Prism-PET detector modules arranged in a conformal decagon geometry, which reduces the partial volume effect and enables accurate quantification of radiotracer uptake in small subcortical nuclei.

MEDICAL PHYSICS (2022)

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Article Multidisciplinary Sciences

[18F]Difluorocarbene for positron emission tomography

Jeroen B. I. Sap et al.

Summary: This study introduces a novel [F-18] difluorocarbene reagent, which resolves the issue of high molar activity in F-18 difluoromethylated molecules by incorporating carbene chemistry, showcasing its versatility and ease of access.

NATURE (2022)

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Article Biotechnology & Applied Microbiology

Spatiotemporal multiplexed immunofluorescence imaging of living cells and tissues with bioorthogonal cycling of fluorescent probes

Jina Ko et al.

Summary: SAFE is a method for comprehensive longitudinal imaging of living cells using immunofluorescence, allowing multiparameter temporal and spatial imaging. It is non-toxic and functional in various living samples.

NATURE BIOTECHNOLOGY (2022)

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Review Biotechnology & Applied Microbiology

The emerging role of mass spectrometry-based proteomics in drug discovery

Felix Meissner et al.

Summary: This Review discusses the potential of proteomics and chemoproteomics approaches in drug discovery, specifically in target identification, validation, and identification of safety hazards. The advancements in biochemical methods and mass spectrometry-based proteomics have allowed for a better understanding of disease mechanisms and the development of targeted drugs.

NATURE REVIEWS DRUG DISCOVERY (2022)

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Article Engineering, Biomedical

Prospective testing of clinical Cerenkov luminescence imaging against standard-of-care nuclear imaging for tumour location

Edwin C. Pratt et al.

Summary: In this study, a clinical CLI fiberscope with a lightproof enclosure was developed and successfully tested using five different radiotracers. In an observational prospective trial involving 96 patients, CLI demonstrated an acceptable level of agreement with standard-of-care imaging for tumour location. CLI correlated with the concentration of radioactive activity and captured therapeutically relevant information.

NATURE BIOMEDICAL ENGINEERING (2022)

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Review Engineering, Biomedical

Multiplexed imaging in oncology

Chrysafis Andreou et al.

Summary: In oncology, clinical molecular imaging technologies play an important role in diagnosing patients, assessing treatment efficacy, and monitoring disease recurrence. Multiplexed methods that detect multiple disease-specific biomarkers simultaneously can improve the accuracy and specificity of these technologies. This review discusses established and emerging multiplexed imaging techniques and highlights the advances in radiology made possible by multiplexed imaging.

NATURE BIOMEDICAL ENGINEERING (2022)

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Review Medicine, General & Internal

PET Molecular Imaging in Drug Development: The Imaging and Chemistry Perspective

Sridhar Goud Nerella et al.

Summary: Positron emission tomography with selective radioligands plays a significant role in drug discovery and development by providing target-specific information, revealing disease progression, and advancing clinical investigation.

FRONTIERS IN MEDICINE (2022)

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Article Multidisciplinary Sciences

A fluorogenic probe for predicting treatment response in non-small cell lung cancer with EGFR-activating mutations

Hui Deng et al.

Summary: In this study, the authors present a fluorescence-activated cell sorting assay to identify activating EGFR mutations in lung cancer patients and demonstrate its utility in predicting response to EGFR-tyrosine kinase inhibitors.

NATURE COMMUNICATIONS (2022)

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Review Medicine, General & Internal

Development, Implementation and Application of Confocal Laser Endomicroscopy in Brain, Head and Neck Surgery-A Review

Irini Kakaletri et al.

Summary: The importance of visualization methods, histopathology, and surgical resection in tumor diagnosis and treatment are emphasized in this review, particularly in the context of Confocal Laser Endomicroscopy (CLE).

DIAGNOSTICS (2022)

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Article Multidisciplinary Sciences

Small molecule photocatalysis enables drug target identification via energy transfer

Aaron D. Trowbridge et al.

Summary: More than half of new therapeutic approaches fail in clinical trials due to a lack of target validation. This study presents a photocatalytic small molecule target identification platform that uses catalytic signal amplification to achieve quantitative target identification.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2022)

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Article Chemistry, Multidisciplinary

Raman Spectroscopy for Chemical Biology Research

Kosuke Dodo et al.

Summary: This article introduces the application of Raman spectroscopy in chemical biology research, including label-free Raman imaging of biomolecules and Raman imaging of small molecules using Raman tags. Raman probes represent the next-generation probes in chemical biology.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2022)

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Article Multidisciplinary Sciences

The E3 ligase adapter cereblon targets the C-terminal cyclic imide degron

Saki Ichikawa et al.

Summary: This study identifies C-terminal cyclic imides as physiological degrons for the ubiquitin E3 ligase substrate adapter cereblon (CRBN). The addition of these degrons induces CRBN-dependent ubiquitination and degradation of proteins. This discovery has significant implications for understanding the physiological and therapeutic engagement of CRBN.

NATURE (2022)

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Review Biotechnology & Applied Microbiology

Advances in covalent drug discovery

Lydia Boike et al.

Summary: Covalent drugs have been widely used for over a century, but recent advances in tools for rational design have led to the successful development of potent and selective inhibitors, such as KRAS(G12C) inhibitors. The use of electrophile-first approaches and the emergence of chemoproteomics platforms have greatly enhanced the discovery and development of covalent drugs.

NATURE REVIEWS DRUG DISCOVERY (2022)

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Article Multidisciplinary Sciences

Structural basis for specific inhibition of the deubiquitinase UCHL1

Christian Grethe et al.

Summary: This study reveals the structural basis for the specific inhibition of UCHL1 and introduces chemogenomic probes that can be used for investigating UCHL1 functions in living cells. Understanding the molecular roles of UCHL1 is important for studying cancer invasiveness and neurodegeneration. The newly developed probes provide valuable tools for cellular investigations of UCHL1.

NATURE COMMUNICATIONS (2022)

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Review Chemistry, Multidisciplinary

Applications of covalent chemistry in targeted protein degradation

Dong Lu et al.

Summary: Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are two exciting strategies in the fields of chemical biology and drug discovery. The emergence of covalent PROTACs, which combine these two strategies, has gained increasing interest in recent years. This review highlights the mechanism and advantages of TCIs and PROTACs, and discusses the recent development of covalent PROTACs using irreversible and reversible covalent chemistry.

CHEMICAL SOCIETY REVIEWS (2022)

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Review Chemistry, Multidisciplinary

Near-infrared (NIR) fluorescence-emitting small organic molecules for cancer imaging and therapy

Hui Li et al.

Summary: Near-infrared (NIR) fluorophores have great potential in tumor imaging and therapy, but non-targeting dyes suffer from low selectivity. Therefore, extensive research efforts have been devoted to developing NIR fluorophores that specifically target tumors, resulting in significant progress.

CHEMICAL SOCIETY REVIEWS (2022)

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Review Chemistry, Multidisciplinary

PROTAC degraders as chemical probes for studying target biology and target validation

Vaclav Nemec et al.

Summary: Small molecule degraders called PROTACs have emerged as a promising pharmacological modality for protein degradation and have the potential to expand the proteome that can be targeted by small molecules. Their development and characterization require additional assays and specific quality criteria compared to conventional chemical probes. This review discusses recent progress in the development of assay systems and suggests a set of criteria for high-quality PROTACs as chemical probes.

CHEMICAL SOCIETY REVIEWS (2022)

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Review Biochemistry & Molecular Biology

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

Ming He et al.

Summary: PROTACs technology is a promising protein-degradation strategy with potential clinical applications and valuable tools for biological research. The field of protein degradation has witnessed rapid development in the past two years, with an increase in research papers and the emergence of small-molecule degraders for clinical use. This article reviews representative PROTACs published in 2020-2021 and briefly discusses the challenges in the field.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2022)

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Review Biochemistry & Molecular Biology

Targeted protein degradation: mechanisms, strategies and application

Lin Zhao et al.

Summary: Traditional drug discovery focuses on direct regulation of protein activity. However, the emerging targeted protein degradation (TPD) technologies, such as PROTAC, provide potential approaches to remove disease-associated proteins by utilizing cells' degradation machinery. These TPD strategies, including molecular glue, LYTAC, and AbTAC, expand the scope of TPD and offer fresh insights into drug discovery.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2022)

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Review Chemistry, Multidisciplinary

Design of Nuclear Magnetic Resonance Molecular Probes for Hyperpolarized Bioimaging

Yohei Kondo et al.

Summary: Nuclear hyperpolarization is a method to enhance the sensitivity of NMR spectroscopy, allowing for highly sensitive biomedical molecular imaging. Recent development of molecular probes for hyperpolarized in vivo analysis has shown the unique metabolic and physiological information that this technique can provide.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Review Chemistry, Multidisciplinary

Molecular Engineering of NIR-II Fluorophores for Improved Biomedical Detection

Zuhai Lei et al.

Summary: The development of fluorophores for the NIR-II window is a significant and vibrant field in chemistry, biology, and engineering, with wavelength, brightness, and stability being crucial factors. Progress has been made in synthesizing D-A-D and D-pi-A fluorophores, as well as constructing off-on and ratiometric probes.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Article Biochemistry & Molecular Biology

SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging

Wioletta Rut et al.

Summary: A team of researchers synthesized a new type of antiviral agent, demonstrating through experiments its high efficacy in inhibiting SARS-CoV-2 with a low effective concentration, providing new insights for antiviral treatment. By observing the active SARS-CoV-2 M-pro in the cells of patients infected with COVID-19, important clues were provided for the design of antiviral drugs and diagnostic tests.

NATURE CHEMICAL BIOLOGY (2021)

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Article Chemistry, Multidisciplinary

A Palette of Minimally Tagged Sucrose Analogues for Real-Time Raman Imaging of Intracellular Plant Metabolism

Fabio de Moliner et al.

Summary: This study successfully synthesized sucrose analogues with Raman tags and demonstrated their recognition and Raman intensity in live cells, further showcasing the application of compound 6 for real-time monitoring of sucrose uptake and intracellular localization in live plant cells using Raman microscopy.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Review Hematology

Incorporating acalabrutinib, a selective next-generation Bruton tyrosine kinase inhibitor, into clinical practice for the treatment of haematological malignancies

Alexey V. Danilov et al.

Summary: Advancements in understanding the disease progression of haematological malignancies have led to the development of novel targeted therapies, such as acalabrutinib, which show promise in improving treatment outcomes for patients with CLL/SLL and MCL. With its high selectivity and potential to reduce off-target toxicity, it has gained accelerated approval for clinical use and has demonstrated efficacy in phase 3 trials.

BRITISH JOURNAL OF HAEMATOLOGY (2021)

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Article Multidisciplinary Sciences

Metallaphotoredox aryl and alkyl radiomethylation for PET ligand discovery

Robert W. Pipal et al.

Summary: By utilizing a versatile and rapid metallaphotoredox-catalysed method, both tritium and carbon-11 can be efficiently introduced into pharmaceutical precursors bearing aryl and alkyl bromides, simplifying the synthesis of radioligands and expanding their applicability. This technique has direct utility for preclinical PET imaging and translation to automated radiosynthesis, demonstrating its potential for routine radiotracer production in human clinical imaging.

NATURE (2021)

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Article Biotechnology & Applied Microbiology

Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries

Miljan Kuljanin et al.

Summary: This study presents a redesigned workflow called streamlined cysteine activity-based protein profiling (SLC-ABPP) for measuring amino acid side-chain reactivity, which significantly improves sample throughput. The method has been successfully applied to identify proteome-wide targets of various covalent inhibitors, while also creating a resource of cysteine reactivity data for further research.

NATURE BIOTECHNOLOGY (2021)

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Article Biochemical Research Methods

Cell surface thermal proteome profiling tracks perturbations and drug targets on the plasma membrane

Mathias Kalxdorf et al.

Summary: This study introduces cell surface thermal proteome profiling for comprehensive characterization of protein changes induced by ligands. It reveals drug binding to receptors, remodeling of T cell receptor complexes, and a competition-based method to measure G-protein-coupled receptor antagonist engagement. Remodeling of the plasma membrane proteome in response to a TGFB receptor inhibitor explains the antimetastatic effects of the drug.

NATURE METHODS (2021)

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Article Biochemical Research Methods

Click-ExM enables expansion microscopy for all biomolecules

De-en Sun et al.

Summary: click-ExM integrates click labeling and fluorescent staining to enable nanoscale imaging of various biomolecules, such as lipids, glycans, proteins, DNA, RNA, and small molecules. It is applicable in cell culture systems and tissue imaging, and compatible with signal-amplification techniques and two-color imaging. Click-ExM provides a convenient and versatile method for super-resolution imaging.

NATURE METHODS (2021)

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Article Oncology

Liquid biopsy enters the clinic - implementation issues and future challenges

Michail Ignatiadis et al.

Summary: The approval of liquid biopsy assays for detecting genetic alterations in plasma cell-free DNA has marked a tipping point for the clinical use of this technology, especially in patients with advanced-stage cancer. The next frontier is likely to be the systemic treatment of patients with 'ctDNA relapse' and other potential future applications include cancer screening and diagnosis.

NATURE REVIEWS CLINICAL ONCOLOGY (2021)

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Article Nanoscience & Nanotechnology

Extracellular vesicle drug occupancy enables real-time monitoring of targeted cancer therapy

Sijun Pan et al.

Summary: The platform developed in this study leverages circulating extracellular vesicles for activity-based assessment of tumour-specific drug-target interactions and can be used for clinical cancer treatment monitoring.

NATURE NANOTECHNOLOGY (2021)

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Article Chemistry, Multidisciplinary

Strategic Design of Catalytic Lysine-Targeting Reversible Covalent BCR-ABL Inhibitors

David Quach et al.

Summary: In this study, a carbonyl boronic acid warhead was utilized to design BCR-ABL inhibitors, targeting the catalytic lysine with improved potency against ABL kinases. Selectivity of these inhibitors largely depends on molecular recognition of the non-covalent pharmacophore, and insights into the interaction of the warhead with the catalytic lysine were provided through cocrystal structures. The off-target evaluation of compounds was performed using label-free mass spectrometry in different mammalian cells.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Article Biochemistry & Molecular Biology

Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo

Christian Dubiella et al.

Summary: Through screening an electrophilic fragment library, a highly selective and effective Pin1 inhibitor named Sulfopin was developed, showing promising anti-tumor activity by downregulating c-Myc target genes, slowing tumor progression, and improving survival rates in murine models of neuroblastoma and pancreatic cancer.

NATURE CHEMICAL BIOLOGY (2021)

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Article Multidisciplinary Sciences

Catalytic amplification by transition-state molecular switches for direct and sensitive detection of SARS-CoV-2

Noah R. Sundah et al.

Summary: CATCH is a molecular nanotechnology that enables direct and sensitive detection of viral RNA targets in clinical samples, achieving superior performance and versatile implementation.

SCIENCE ADVANCES (2021)

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Article Biochemistry & Molecular Biology

A Comparison of Two Stability Proteomics Methods for Drug Target Identification in OnePot 2D Format

Yingrong Xu et al.

Summary: Stability proteomics techniques have emerged as an attractive alternative in drug target engagement studies, with SPROX and TPP being representative methods. The adoption of the OnePot strategy has increased throughput and efficiency, with the OnePot 2D format offering improved analysis specificity. However, there is still a lack of systematic evaluation of the OnePot 2D format and a comparison between SPROX and TPP.

ACS CHEMICAL BIOLOGY (2021)

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Article Chemistry, Multidisciplinary

Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs

Robert P. Law et al.

Summary: This study introduced a novel FAK-degrading PROTAC, GSK215, designed based on VHL E3 ligase and the FAK inhibitor VS-4718, showing promising potential for a differentiated clinical strategy in cancer treatment compared to conventional FAK inhibition. The highly cooperative FAK-GSK215-VHL ternary complex revealed by X-ray crystallography provided insights into the molecular basis of the compound's efficacy. In mouse models, GSK215 demonstrated rapid and prolonged FAK degradation, highlighting its potential as a valuable tool for studying FAK-degradation biology in vivo.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2021)

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Article Cell Biology

Quantitative proteomics identifies the core proteome of exosomes with syntenin-1 as the highest abundant protein and a putative universal biomarker

Fernanda G. Kugeratski et al.

Summary: The study used an unbiased and quantitative proteomic approach to identify core constituents of exosomes, with syntenin-1 identified as a potential universal biomarker. A comprehensive quantitative atlas of core proteins ubiquitous to exosomes was provided, highlighting the potential use of syntenin-1 as a putative universal biomarker for exosomes.

NATURE CELL BIOLOGY (2021)

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Review Neurosciences

Expansion microscopy: A powerful nanoscale imaging tool for neuroscientists

Brendan R. Gallagher et al.

Summary: One of the biggest challenges in neuroscience is understanding how molecules and neuronal circuitry give rise to behaviors, and how their dysfunction leads to neurological diseases. While light microscopy is a crucial tool for studying neural molecules and circuits, the diffraction limit hinders detailed characterization of subcellular structures and nanoscopic organizations. Super-resolution microscopy methods have been developed to bypass this limitation, allowing highly resolved imaging in the nanometer range. Expansion Microscopy (ExM) has emerged as a promising solution to surpass the diffraction limit by physically enlarging biological specimens, providing a powerful tool for studying neural systems at the nanoscale.

NEUROBIOLOGY OF DISEASE (2021)

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Review Cell Biology

Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation

Ming He et al.

Summary: PROTAC is a new technology for inducing protein degradation using small molecules, which shows advantages in overcoming tumor resistance, affecting non-enzymatic functions of target proteins, degrading undruggable targets, and providing rapid and reversible chemical knockout tools. However, it also faces challenges and issues as a rapidly developing new chemical biology technology.

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2021)

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Article Chemistry, Multidisciplinary

Intramolecular charge transfer enhancing strategy based MAO-A specific two-photon fluorescent probes for glioma cell/tissue imaging

Haixiao Fang et al.

Summary: The study introduces a series of MAO-A specific fluorescent probes and demonstrates the selective imaging of endogenous MAO-A activity in different biological samples using these probes, offering new tools for visual detection of glioma.

CHEMICAL COMMUNICATIONS (2021)

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Article Chemistry, Multidisciplinary

Selective Mitochondrial Protein Labeling Enabled by Biocompatible Photocatalytic Reactions inside Live Cells

Haoyan Wang et al.

Summary: Biocompatible photocatalytic azide conjugation reaction enables selective labeling of mitochondrial proteins inside live cells, mapping dynamic mitochondrial proteome changes with high temporal-spatial precision.

JACS AU (2021)

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Review Chemistry, Multidisciplinary

Small-molecule fluorescence-based probes for interrogating major organ diseases

Hai-Hao Han et al.

Summary: This tutorial review discusses the importance of chemical tools in real-time monitoring of organ function and visualization of organ-related processes at the cellular level in biological research. It highlights the potential of small-molecule fluorescent probes in advancing the understanding of organ-related diseases and emphasizes the need for probes with high sensitivity, low limit of detection, fast response times, and appropriate biocompatibility.

CHEMICAL SOCIETY REVIEWS (2021)

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Review Oncology

Advancing targeted protein degradation for cancer therapy

Brandon Dale et al.

Summary: The development of small-molecule degraders such as proteolysis-targeting chimeras (PROTACs) has enabled the targeting of previously considered undruggable oncoproteins. This review discusses recent advances in the field, with a focus on opportunities and challenges for future development.

NATURE REVIEWS CANCER (2021)

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Review Materials Science, Multidisciplinary

Emerging applications of stimulated Raman scattering microscopy in materials science

Qian Cheng et al.

Summary: Stimulated Raman scattering (SRS) is a powerful chemical imaging technique with high chemical, spatial, and temporal resolution, suitable for applications in materials science and biomedicine. The high-speed and high-chemical sensitivity of SRS have attracted attention from the materials science community and have been successfully applied in various areas, such as 2D materials, energy storage, and polymer chemistry.

MATTER (2021)

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Review Chemistry, Multidisciplinary

Recent advances in activity-based probes (ABPs) and affinity-based probes (AfBPs) for profiling of enzymes

Haixiao Fang et al.

Summary: Activity-based protein profiling (ABPP) is a technique that utilizes selective chemical probes to monitor protein activity, revealing enzyme-substrate interactions and providing information on catalytic activity changes. ABPP can annotate new functions and substrates of enzymes, allowing real-time monitoring of enzyme cellular location.

CHEMICAL SCIENCE (2021)

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Review Chemistry, Multidisciplinary

Stimulus-cleavable chemistry in the field of controlled drug delivery

Yufei Xue et al.

Summary: This review summarizes the recent advances in stimulus-cleavable linkers and their biological applications, highlighting the feasibility of extending their applications to various nanoscale drug carriers. It also provides general design guidelines for incorporating stimulus-cleavable linkers into nanocarrier-based drug delivery systems, aiming to spark new ideas and applications in this field.

CHEMICAL SOCIETY REVIEWS (2021)

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Review Chemistry, Multidisciplinary

Two-photon small-molecule fluorescence-based agents for sensing, imaging, and therapy within biological systems

Luling Wu et al.

Summary: This tutorial review explores recent advances in the design, construction, and application of two-photon excited fluorescence (TPEF)-based small-molecule probes, discussing advantages, two-photon fluorophores, design strategies, and various applications including photodynamic therapy.

CHEMICAL SOCIETY REVIEWS (2021)

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Review Biochemistry & Molecular Biology

Recent advances in identifying protein targets in drug discovery

Jaeyoung Ha et al.

Summary: Phenotype-based screening is a promising method for discovering first-in-class therapeutics, but understanding the mode of action has been a bottleneck for drug discovery. Recent strategies including covalent conjugation and label-free target identification have emerged to overcome limitations in target protein identification, leading to significant advancements in the field.

CELL CHEMICAL BIOLOGY (2021)

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Article Radiology, Nuclear Medicine & Medical Imaging

Development of a Novel Histone Deacetylase-Targeted Near-Infrared Probe for Hepatocellular Carcinoma Imaging and Fluorescence Image-Guided Surgery

Chu Tang et al.

MOLECULAR IMAGING AND BIOLOGY (2020)

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Article Chemistry, Multidisciplinary

Rational Design of a Two-Photon Fluorogenic Probe for Visualizing Monoamine Oxidase A Activity in Human Glioma Tissues

Haixiao Fang et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

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Review Biochemistry & Molecular Biology

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

George M. Burslem et al.

CELL (2020)

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Click Chemistry in Proteomic Investigations

Christopher G. Parker et al.

CELL (2020)

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Fluorine-18: A radionuclide with diverse range of radiochemistry and synthesis strategies for target based PET diagnosis

Nerella Sridhar Goud et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Article Biotechnology & Applied Microbiology

Identifying drug targets in tissues and whole blood with thermal-shift profiling

Jessica Perrin et al.

NATURE BIOTECHNOLOGY (2020)

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Discovery of a first-in-class EZH2 selective degrader

Anqi Ma et al.

NATURE CHEMICAL BIOLOGY (2020)

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A general strategy to develop cell permeable and fluorogenic probes for multicolour nanoscopy

Lu Wang et al.

NATURE CHEMISTRY (2020)

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Visualization of AMPA receptors in living human brain with positron emission tomography

Tomoyuki Miyazaki et al.

NATURE MEDICINE (2020)

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The biology, function, and biomedical applications of exosomes

Raghu Kalluri et al.

SCIENCE (2020)

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Microenvironment mapping via Dexter energy transfer on immune cells

Jacob B. Geri et al.

SCIENCE (2020)

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First-in-human liver-tumour surgery guided by multispectral fluorescence imaging in the visible and near-infrared-I/II windows

Zhenhua Hu et al.

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Safety and Feasibility of PARP1/2 Imaging with 18F-PARPi in Patients with Head and Neck Cancer

Heiko Schoder et al.

CLINICAL CANCER RESEARCH (2020)

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Feasibility of blood testing combined with PET-CT to screen for cancer and guide intervention

Anne Marie Lennon et al.

SCIENCE (2020)

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PET ligands [18F]LSN3316612 and [11C]LSN3316612 quantify O-linked-β-N-acetyl-glucosamine hydrolase in the brain

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SCIENCE TRANSLATIONAL MEDICINE (2020)

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2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells

Nan Ma et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)

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TMTpro reagents: a set of isobaric labeling mass tags enables simultaneous proteome-wide measurements across 16 samples

Jiaming Li et al.

NATURE METHODS (2020)

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Article Engineering, Biomedical

Validation of the use of a fluorescent PARP1 inhibitor for the detection of oral, oropharyngeal and oesophageal epithelial cancers

Susanne Kossatz et al.

NATURE BIOMEDICAL ENGINEERING (2020)

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Review Oncology

Overview of multiplex immunohistochemistry/immunofluorescence techniques in the era of cancer immunotherapy

Wei Chang Colin Tan et al.

CANCER COMMUNICATIONS (2020)

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Article Biochemistry & Molecular Biology

Novel Tetrafunctional Probes Identify Target Receptors and Binding Sites of Small-Molecule Drugs from Living Systems

Rin Miyajima et al.

ACS CHEMICAL BIOLOGY (2020)

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Article Biochemistry & Molecular Biology

An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells

Ekaterina V. Vinogradova et al.

CELL (2020)

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Article Engineering, Biomedical

Purification of protein therapeutics via high-affinity supramolecular host-guest interactions

Jaeyeon An et al.

NATURE BIOMEDICAL ENGINEERING (2020)

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Developing bioorthogonal probes to span a spectrum of reactivities

Sean S. Nguyen et al.

NATURE REVIEWS CHEMISTRY (2020)

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Quantitative Drug Dynamics Visualized by Alkyne-Tagged Plasmonic-Enhanced Raman Microscopy

Kota Koike et al.

ACS NANO (2020)

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Lysosome-targeting chimaeras for degradation of extracellular proteins

Steven M. Banik et al.

NATURE (2020)

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Article Biochemistry & Molecular Biology

Discovery of small-molecule enzyme activators by activity-based protein profiling

Bernard P. Kok et al.

NATURE CHEMICAL BIOLOGY (2020)

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Article Chemistry, Multidisciplinary

Small-Molecule Activity-Based Probe for Monitoring Ubiquitin C-Terminal Hydrolase L1 (UCHL1) Activity in Live Cells and Zebrafish Embryos

Raymond Kooij et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)

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Article Chemistry, Multidisciplinary

A Visible and Near-Infrared Light Activatable Diazocoumarin Probe for Fluorogenic Protein Labeling in Living Cells

Sheng-Yao Dai et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2020)

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Article Chemistry, Multidisciplinary

Using sulfuramidimidoyl fluorides that undergo sulfur(vi) fluoride exchange for inverse drug discovery

Gabriel J. Brighty et al.

NATURE CHEMISTRY (2020)

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Article Multidisciplinary Sciences

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

Wen-Hao Guo et al.

NATURE COMMUNICATIONS (2020)

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Article Biochemistry & Molecular Biology

Recent developments in bioorthogonal chemistry and the orthogonality within

Mike L.W.J. Smeenk et al.

CURRENT OPINION IN CHEMICAL BIOLOGY (2020)

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Review Respiratory System

PARP inhibitors for small cell lung cancer and their potential for integration into current treatment approaches

Ranya Barayan et al.

JOURNAL OF THORACIC DISEASE (2020)

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Sensors for In Situ Real-Time Fluorescence Imaging of Enzymes

Xiaofeng Wu et al.

CHEM (2020)

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Review Chemistry, Multidisciplinary

Bioapplications of small molecule Aza-BODIPY: from rational structural design to in vivo investigations

Zhenxiong Shi et al.

CHEMICAL SOCIETY REVIEWS (2020)

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The evolving translational potential of small extracellular vesicles in cancer

Andreas Moller et al.

NATURE REVIEWS CANCER (2020)

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Fine-tuning the electronic structure of heavy-atom-freeBODIPYphotosensitizers for fluorescence imaging and mitochondria-targeted photodynamic therapy

Sujie Qi et al.

CHEMICAL SCIENCE (2020)

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Review Oncology

Circulating tumor DNA and liquid biopsy in oncology

David W. Cescon et al.

NATURE CANCER (2020)

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Article Materials Science, Multidisciplinary

Dual-Selective Magnetic Analysis of Extracellular Vesicle Glycans

Zhigang Wang et al.

MATTER (2020)

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Review Chemistry, Multidisciplinary

Chemistry for Positron Emission Tomography: Recent Advances in 11C-, 18F-, 13N-, and 15O-Labeling Reactions

Xiaoyun Deng et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2019)

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Article Radiology, Nuclear Medicine & Medical Imaging

68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers

Frederik L. Giesel et al.

JOURNAL OF NUCLEAR MEDICINE (2019)

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Review Oncology

The beginning of the end for conventional RECIST - novel therapies require novel imaging approaches

Mirjam Gerwing et al.

NATURE REVIEWS CLINICAL ONCOLOGY (2019)

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Article Multidisciplinary Sciences

Mobile platform for rapid sub-picogram-per-milliliter, multiplexed, digital droplet detection of proteins

Venkata Yelleswarapu et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

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Article Multidisciplinary Sciences

Subtyping of circulating exosome-bound amyloid β reflects brain plaque deposition

Carine Z. J. Lim et al.

NATURE COMMUNICATIONS (2019)

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Article Chemistry, Multidisciplinary

Stable, Reactive, and Orthogonal Tetrazines: Dispersion Forces Promote the Cycloaddition with Isonitriles

Julian Tu et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2019)

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Article Oncology

Discovery and Characterization of SY-1365, a Selective, Covalent Inhibitor of CDK7

Shanhu Hu et al.

CANCER RESEARCH (2019)

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Correction Radiology, Nuclear Medicine & Medical Imaging

PET of Poly (ADP-Ribose) Polymerase Activity in Cancer: Preclinical Assessment and First In-Human Studies (vol 282, pg 453, 2017)

Loren S. Michel et al.

RADIOLOGY (2019)

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Review Radiology, Nuclear Medicine & Medical Imaging

PSMA-Targeted Radiopharmaceuticals for Imaging and Therapy

Hans-Juergen Wester et al.

SEMINARS IN NUCLEAR MEDICINE (2019)

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Molecular conjugation using non-covalent click chemistry

Cynthia L. Schreiber et al.

NATURE REVIEWS CHEMISTRY (2019)

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Cellular Imaging Using Stimulated Raman Scattering Microscopy

Andrew H. Hill et al.

ANALYTICAL CHEMISTRY (2019)

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Review Radiology, Nuclear Medicine & Medical Imaging

Two decades of SPECT/CT - the coming of age of a technology: An updated review of literature evidence

Ora Israel et al.

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2019)

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Article Chemistry, Multidisciplinary

Chemoproteomic Method for Profiling Inhibitor-Bound Kinase Complexes

Linglan Fang et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2019)

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Article Biochemistry & Molecular Biology

Development of targeted protein degradation therapeutics

Philip P. Chamberlain et al.

NATURE CHEMICAL BIOLOGY (2019)

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Biological imaging of chemical bonds by stimulated Raman scattering microscopy

Fanghao Hu et al.

NATURE METHODS (2019)

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Article Nanoscience & Nanotechnology

Bio-orthogonal Supramolecular Latching inside Live Animals and Its Application for in Vivo Cancer Imaging

Meng Li et al.

ACS APPLIED MATERIALS & INTERFACES (2019)

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Chemical Proteomic Profiling of Lysophosphatidic Acid-Binding Proteins

Xuejiao Dong et al.

ANALYTICAL CHEMISTRY (2019)

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A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family

Emma K. Grant et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2019)

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Article Chemistry, Multidisciplinary

Light-Induced Protein Degradation with Photocaged PROTACs

Gang Xue et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2019)

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Ultrasensitive, multiplexed chemoproteomic profiling with soluble activity-dependent proximity ligation

Gang Li et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

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Cellular quality control by the ubiquitin-proteasome system and autophagy

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SCIENCE (2019)

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Review Chemistry, Analytical

Recent Advances in Design of Fluorescence-Based Assays for High-Throughput Screening

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ANALYTICAL CHEMISTRY (2019)

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Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

Matthias Gehringer et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

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Article Biochemistry & Molecular Biology

Selective and reversible modification of kinase cysteines with chlorofluoroacetamides

Naoya Shindo et al.

NATURE CHEMICAL BIOLOGY (2019)

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Article Biochemistry & Molecular Biology

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

Sajid Khan et al.

NATURE MEDICINE (2019)

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Meeting Abstract Oncology

ARV-471, an oral estrogen receptor PROTAC degrader for breast cancer

J. J. Flanagan et al.

CANCER RESEARCH (2019)

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Target engagement approaches for pharmacological evaluation in animal models

James E. Kath et al.

CHEMICAL COMMUNICATIONS (2019)

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The evidence framework for precision cancer medicine

Jeffrey A. Moscow et al.

NATURE REVIEWS CLINICAL ONCOLOGY (2018)

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Article Radiology, Nuclear Medicine & Medical Imaging

18F-FPYBF-2, a new F-18-labelled amyloid imaging PET tracer: first experience in 61 volunteers and 55 patients with dementia

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ANNALS OF NUCLEAR MEDICINE (2018)

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Article Biochemistry & Molecular Biology

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation

Alexandru D. Buhimschi et al.

BIOCHEMISTRY (2018)

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Review Chemistry, Multidisciplinary

New Technologies for Analysis of Extracellular Vesicles

Huilin Shao et al.

CHEMICAL REVIEWS (2018)

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Review Chemistry, Multidisciplinary

Long-Lived Emissive Probes for Time-Resolved Photoluminescence Bioimaging and Biosensing

Kenneth Yin Zhang et al.

CHEMICAL REVIEWS (2018)

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Progress with covalent small-molecule kinase inhibitors

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DRUG DISCOVERY TODAY (2018)

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The future of blood-based biomarkers for the early detection of breast cancer

Sau Yeen Loke et al.

EUROPEAN JOURNAL OF CANCER (2018)

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Fishing for Drug Targets: A Focus on Diazirine Photoaffinity Probe Synthesis

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JOURNAL OF MEDICINAL CHEMISTRY (2018)

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Article Radiology, Nuclear Medicine & Medical Imaging

Molecular Imaging in Cancer Drug Development

Stijn J. H. Waaijer et al.

JOURNAL OF NUCLEAR MEDICINE (2018)

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Unraveling Tetrazine-Triggered Bioorthogonal Elimination Enables Chemical Tools for Ultrafast Release and Universal Cleavage

Jonathan C. T. Carlson et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2018)

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Article Biochemistry & Molecular Biology

The dTAG system for immediate and target-specific protein degradation

Behnam Nabet et al.

NATURE CHEMICAL BIOLOGY (2018)

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Article Biochemistry & Molecular Biology

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Lara N. Gechijian et al.

NATURE CHEMICAL BIOLOGY (2018)

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Review Cell Biology

Shedding light on the cell biology of extracellular vesicles

Guillaume van Niel et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2018)

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Article Multidisciplinary Sciences

Detection and localization of surgically resectable cancers with a multi-analyte blood test

Joshua D. Cohen et al.

SCIENCE (2018)

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Article Cell Biology

A PET imaging approach for determining EGFR mutation status for improved lung cancer patient management

Xilin Sun et al.

SCIENCE TRANSLATIONAL MEDICINE (2018)

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Supramolecular latching system based on ultrastable synthetic binding pairs as versatile tools for protein imaging

Kyung Lock Kim et al.

NATURE COMMUNICATIONS (2018)

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Article Multidisciplinary Sciences

Target engagement imaging of PARP inhibitors in small-cell lung cancer

Brandon Carney et al.

NATURE COMMUNICATIONS (2018)

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Article Multidisciplinary Sciences

Heterogeneity in tumor chromatin-doxorubicin binding revealed by in vivo fluorescence lifetime imaging confocal endomicroscopy

Hugh Sparks et al.

NATURE COMMUNICATIONS (2018)

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Article Clinical Neurology

Association Between Amyloid and Tau Accumulation in Young Adults With Autosomal Dominant Alzheimer Disease

Yakeel T. Quiroz et al.

JAMA NEUROLOGY (2018)

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Review Nanoscience & Nanotechnology

Nanoplasmonic optical antennas for life sciences and medicine

Hongbao Xin et al.

NATURE REVIEWS MATERIALS (2018)

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Meeting Abstract Oncology

ARV-110: An androgen receptor PROTAC degrader for prostate cancer

Taavi Neklesa et al.

CANCER RESEARCH (2018)

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Article Chemistry, Medicinal

Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility

Matthew R. Naylor et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

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Article Biochemistry & Molecular Biology

Selective blockade of the lyso-PS lipase ABHD12 stimulates immune responses in vivo

Daisuke Ogasawara et al.

NATURE CHEMICAL BIOLOGY (2018)

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Article Genetics & Heredity

Genetics of blood lipids among ∼300,000 multi-ethnic participants of the Million Veteran Program

Derek Klarin et al.

NATURE GENETICS (2018)

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Article Chemistry, Multidisciplinary

A Vinyl Sulfone-Based Fluorogenic Probe Capable of Selective Labeling of PHGDH in Live Mammalian Cells

Sijun Pan et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2018)

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Article Chemistry, Medicinal

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions

Paul A. Jackson et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

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Article Biochemistry & Molecular Biology

Quantitating drug-target engagement in single cells in vitro and in vivo

J. Matthew Dubach et al.

NATURE CHEMICAL BIOLOGY (2017)

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Article Oncology

RECIST-learning from the past to build the future

Saskia Litiere et al.

NATURE REVIEWS CLINICAL ONCOLOGY (2017)

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Review Biotechnology & Applied Microbiology

Induced protein degradation: an emerging drug discovery paradigm

Ashton C. Lai et al.

NATURE REVIEWS DRUG DISCOVERY (2017)

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Article Pharmacology & Pharmacy

Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile

Tjeerd Barf et al.

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Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes

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JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2017)

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Article Biotechnology & Applied Microbiology

Cell-type-specific metabolic labeling of nascent proteomes in vivo

Beatriz Alvarez-Castelao et al.

NATURE BIOTECHNOLOGY (2017)

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Global profiling of lysine reactivity and ligandability in the human proteome

Stephan M. Hacker et al.

NATURE CHEMISTRY (2017)

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Article Biochemical Research Methods

Measuring protein structural changes on a proteome-wide scale using limited proteolysis-coupled mass spectrometry

Simone Schopper et al.

NATURE PROTOCOLS (2017)

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Article Radiology, Nuclear Medicine & Medical Imaging

Nuclear data for production and medical application of radionuclides: Present status and future needs

Syed M. Qaim

NUCLEAR MEDICINE AND BIOLOGY (2017)

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Review Multidisciplinary Sciences

The cancer epigenome: Concepts, challenges, and therapeutic opportunities

Mark A. Dawson

SCIENCE (2017)

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Click chemistry enables preclinical evaluation of targeted epigenetic therapies

Dean S. Tyler et al.

SCIENCE (2017)

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Article Multidisciplinary Sciences

Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds

Yong Yao Loh et al.

SCIENCE (2017)

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Article Multidisciplinary Sciences

Redox-based reagents for chemoselective methionine bioconjugation

Shixian Lin et al.

SCIENCE (2017)

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Article Multidisciplinary Sciences

Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474

Annelot C. M. van Esbroeck et al.

SCIENCE (2017)

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Article Cell Biology

Clinical chemoproteomics - Opportunities and obstacles

Lyn H. Jones et al.

SCIENCE TRANSLATIONAL MEDICINE (2017)

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The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

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