☆ 4.5 Review

Open resources for chemical probes and their implications for future drug discovery

EXPERT OPINION ON DRUG DISCOVERY (2023)

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Article Chemistry, Medicinal

Chemistry42: An AI-Driven Platform for Molecular Design and Optimization

Yan A. Ivanenkov et al.

Summary: Chemistry42 is a software platform that combines Artificial Intelligence techniques with computational and medicinal chemistry methodologies for de novo small molecule design and optimization. It efficiently generates novel molecular structures with optimized properties, which are validated in both in vitro and in vivo studies. Chemistry42 is part of Insilico Medicine's Pharma.ai drug discovery suite, along with PandaOmics for target discovery and multiomics data analysis, and inClinico for data-driven forecast of a clinical trial's probability of success.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2023)

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Review Biochemistry & Molecular Biology

The Chemical Probes Portal: an expert review-based public resource to empower chemical probe assessment, selection and use

Albert A. Antolin et al.

Summary: The Chemical Probes Portal is a public resource for researchers to select and use high-quality chemical probes. Chemical probes are crucial for protein function research and drug discovery, but the use of low-quality probes has led to erroneous conclusions. The portal provides background, principles, content, and technical development, and encourages researcher involvement.

NUCLEIC ACIDS RESEARCH (2023)

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Review Biochemistry & Molecular Biology

AlphaFold2 and its applications in the fields of biology and medicine

Zhenyu Yang et al.

Summary: AlphaFold2 (AF2) is an AI system that accurately predicts the 3D structures of proteins from amino acid sequences. Its development marks a significant advancement in protein structure prediction and has attracted considerable attention. The release of over 200 million predicted protein structures by AF2 has generated great enthusiasm in the scientific community, particularly in the fields of biology and medicine. AF2 is expected to have a profound impact on structural biology and research areas that require protein structure information.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2023)

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Article Chemistry, Multidisciplinary

Strategies for developing DNA-encoded libraries beyond binding assays

Yiran Huang et al.

Summary: DNA-encoded chemical libraries (DELs) have become a powerful technology in drug discovery, widely adopted in the pharmaceutical industry. Recent advancements have shown the potential of DELs to operate in the complex environment of biological systems.

NATURE CHEMISTRY (2022)

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Review Biotechnology & Applied Microbiology

PROTAC targeted protein degraders: the past is prologue

Miklos Bekes et al.

Summary: Targeted protein degradation (TPD) is a new therapeutic modality that can tackle disease-causing proteins which are difficult to target with conventional small molecules. PROTAC molecules, utilizing the ubiquitin-proteasome system to degrade target proteins, has achieved clinical proof-of-concept and attracted significant industry activity. Future directions include identifying target classes suitable for TPD, expanding the use of ubiquitin ligases for precision medicine, and extending the modality beyond oncology.

NATURE REVIEWS DRUG DISCOVERY (2022)

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Article Biochemical Research Methods

Fast fragment- and compound-screening pipeline at the Swiss Light Source

Jakub W. Kaminski et al.

Summary: Fragment-based drug discovery has been proven to be an effective and efficient method for identifying new chemical scaffolds. X-ray crystallography can be used to validate and develop identified fragments, and recent technological advancements have enabled the development of dedicated platforms for FBDD using X-ray crystallography.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2022)

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Review Biochemistry & Molecular Biology

Validating Small Molecule Chemical Probes for Biological Discovery

Victoria Vu et al.

Summary: This article reviews the technologies used for evaluating the parameters and characteristics of chemical probes, focusing on cellular potency and selectivity. Additionally, it discusses the use of chemical genetic screening for phenotypic characterization of chemical probes and the significance of these data for potential therapeutic targets.

ANNUAL REVIEW OF BIOCHEMISTRY (2022)

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Editorial Material Biotechnology & Applied Microbiology

opnMe.com: a digital initiative for sharing tools with the biomedical research community

Andreas Gollner et al.

Summary: Pharmacological probes are essential for studying disease biology and developing new therapies. The Boehringer Ingelheim open innovation portal opnMe.com addresses the issue of using inadequate molecules by sharing extensively validated probes with the scientific community.

NATURE REVIEWS DRUG DISCOVERY (2022)

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Article Multidisciplinary Sciences

Selective posttranslational inhibition of Ca-V beta(1)-associated voltage-dependent calcium channels with a functionalized nanobody

Travis J. Morgenstern et al.

Summary: This study identifies a nanobody, nb.E8, that selectively binds to the SH3 domain of Ca-V beta(1) and inhibits associated HVACCs. Functionalizing nb.E8 with Nedd4L HECT domain yielded Chisel-1, which eliminates current through Ca-V beta(1)-reconstituted channels and suppresses Ca2+ influx and excitation-transcription coupling in neurons. This research introduces a new method for probing distinctive functions of ion channel auxiliary subunit isoforms, and describes a genetically-encoded HVACC inhibitor with unique properties.

NATURE COMMUNICATIONS (2022)

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Article Biochemistry & Molecular Biology

Rational exploration of fold atlas for human solute carrier proteins

Tengyu Xie et al.

Summary: The solute carrier (SLC) superfamily is the largest group of proteins responsible for transmembrane transport of substances in human cells. This study systematically explored the SLC superfamily and identified at least three new folds, one of which has been experimentally verified in the choline-like transporter family (SLC44). This work lays a foundation and provides important insights for the systematic and comprehensive study of the structure and function of SLC.

STRUCTURE (2022)

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Article Geriatrics & Gerontology

Identification of Therapeutic Targets for Amyotrophic Lateral Sclerosis Using PandaOmics - An AI-Enabled Biological Target Discovery Platform

Frank W. Pun et al.

Summary: In this study, an AI-driven target discovery platform called PandaOmics was used to analyze the expression profiles of CNS samples and direct iPSC-derived motor neurons from public datasets and Answer ALS. The study identified 17 high-confidence and 11 novel therapeutic targets, and verified their therapeutic effects in a fruit fly model. The research provides new insights into ALS pathophysiology and demonstrates the ability of AI to speed up the target discovery process.

FRONTIERS IN AGING NEUROSCIENCE (2022)

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Article Biology

Integrating multi-omics data reveals function and therapeutic potential of deubiquitinating enzymes

Laura M. Doherty et al.

Summary: This study establishes a knowledgebase of DUB activities, co-dependent genes, and substrates, utilizing targeted experiments and systematic mining of functional genomic databases. The findings provide insights into the important role of DUBs in regulating cellular activities and suggest their potential as therapeutic targets for cancer and other diseases.

ELIFE (2022)

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Article Multidisciplinary Sciences

Nanobodies and chemical cross-links advance the structural and functional analysis of PI3K alpha

Jonathan R. Hart et al.

Summary: This study used nanobodies and chemical cross-linking to investigate the identity and positions of flexible domains of PI3K alpha. The application of chemical cross-linking mass spectrometry allowed for the identification of specific domains and their docking positions on the PI3K alpha catalytic core. It was found that binding of nanobodies to PI3K alpha induced changes in enzyme activity and conformation, providing insights into the molecular underpinning of PI3K alpha's flexibility.

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

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Article Biochemistry & Molecular Biology

The era of high-quality chemical probes

Marco. P. P. Licciardello et al.

Summary: Small-molecule chemical probes play a crucial role in studying protein function in cells and organisms. Unfortunately, the use of weak and non-selective small molecules has led to numerous erroneous conclusions in scientific literature. Recently, minimum criteria have been established to encourage the selection and use of high-quality chemical probes.

RSC MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Target 2035-update on the quest for a probe for every protein

Susanne Mueller et al.

Summary: Twenty years after the first draft of the human genome was published, our understanding of the human proteome is still incomplete. The majority of proteins in the human proteome remain uncharacterized, with only a small percentage successfully targeted for drug discovery. Target 2035 aims to bridge this gap by developing new technologies for the entire human proteome by 2035.

RSC MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

PROTAC-DB: an online database of PROTACs

Gaoqi Weng et al.

Summary: PROTACs, a novel therapeutic technology that selectively degrades targeted proteins, has achieved significant progress with two PROTACs in phase I clinical trials. However, the design of PROTACs remains challenging. PROTAC-DB, a web-based database, integrates structural information and experimental data of PROTACs, providing convenient querying and filtering tools for researchers.

NUCLEIC ACIDS RESEARCH (2021)

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Article Biochemistry & Molecular Biology

The BioGRID database: A comprehensive biomedical resource of curated protein, genetic, and chemical interactions

Rose Oughtred et al.

Summary: BioGRID is an open-access database resource that houses protein and genetic interactions from multiple species, serving as a tool for building complex networks to facilitate biomedical discoveries. Curated from primary experimental evidence, BioGRID captures both low-throughput and large high-throughput studies, including protein post-translational modifications and interactions with bioactive small molecules. Additionally, it undertakes themed curation projects in specific aspects of cellular regulation and disease areas.

PROTEIN SCIENCE (2021)

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Review Biochemistry & Molecular Biology

Ubiquitin signaling in neurodegenerative diseases: an autophagy and proteasome perspective

Francois Le Guerroue et al.

Summary: Ubiquitin signaling plays a crucial role in neurodegenerative diseases, primarily associated with degradation signals. Decrease in quality control pathways with age may be a critical factor in the development of neurodegeneration.

CELL DEATH AND DIFFERENTIATION (2021)

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Article Biochemistry & Molecular Biology

RCSB Protein Data Bank: powerful new tools for exploring 3D structures of biological macromolecules for basic and applied research and education in fundamental biology, biomedicine, biotechnology, bioengineering and energy sciences

Stephen K. Burley et al.

Summary: RCSB PDB, as the US data center for the global PDB archive, provides free access to 3D macromolecular structure data for millions of users worldwide, including educators, students, and the general public, integrating over 40 external biodata resources. The redesigned website now features improved search functionality and easier access to PDB data, showcasing new structures relevant to the understanding and addressing of the COVID-19 pandemic.

NUCLEIC ACIDS RESEARCH (2021)

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Article Biochemistry & Molecular Biology

Open Targets Platform: supporting systematic drug-target identification and prioritisation

David Ochoa et al.

Summary: The Open Targets Platform provides a queryable knowledgebase and user interface for systematic target identification and prioritization for drug discovery, continuously improving evidence for target-disease relationships from various data sources. They have developed a new evidence scoring framework, added evaluation of post-marketing adverse drug reactions and target tractability, and optimized user interface and backend technologies to address the challenge of developing effective and safe drugs.

NUCLEIC ACIDS RESEARCH (2021)

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Review Biochemistry & Molecular Biology

Therapeutic Nanobodies Targeting Cell Plasma Membrane Transport Proteins: A High-Risk/High-Gain Endeavor

Raf Van Campenhout et al.

Summary: Cell plasma membrane proteins play a crucial role in cell regulation, with transport proteins facilitating molecule and ion exchange. The dysfunction of these proteins can lead to various human pathologies, making them potential therapeutic targets. Nanobodies show promise in targeting and modulating the activity of these proteins, offering a potential approach in drug development.

BIOMOLECULES (2021)

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Review Multidisciplinary Sciences

Validation of antibodies: Lessons learned from the Common Fund Protein Capture Reagents Program

Ananda L. Roy et al.

Summary: Large-scale generation and validation of protein capture reagents is a technical challenge, with validation being a critical iterative process that yields different results for different uses. Independent community-based validation offers the possibility of transparent data sharing.

SCIENCE ADVANCES (2021)

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Review Pharmacology & Pharmacy

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy

Si-Min Qi et al.

Summary: PROTAC technology is an effective method for degrading target proteins through the ubiquitin-proteasome system, with promising applications in cancer treatment. The first oral PROTACs have shown encouraging results in clinical trials, sparking greater enthusiasm for PROTAC research.

FRONTIERS IN PHARMACOLOGY (2021)

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Review Chemistry, Multidisciplinary

Evolution of the Selection Methods of DNA-Encoded Chemical Libraries

Yinan Song et al.

Summary: DNA-encoded chemical libraries (DELs) have become a major technology platform for ligand discovery in drug discovery and chemical biology research, offering access to vast chemical space at lower cost. While research on selection methods for DELs has been limited, recent developments in solution-phase DEL selections have expanded the application of DELs to complex biological targets.

ACCOUNTS OF CHEMICAL RESEARCH (2021)

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Article Multidisciplinary Sciences

Highly accurate protein structure prediction with AlphaFold

John Jumper et al.

Summary: Proteins are essential for life, and accurate prediction of their structures is a crucial research problem. Current experimental methods are time-consuming, highlighting the need for accurate computational approaches to address the gap in structural coverage. Despite recent progress, existing methods fall short of atomic accuracy in protein structure prediction.

NATURE (2021)

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Article Multidisciplinary Sciences

Highly accurate protein structure prediction for the human proteome

Kathryn Tunyasuvunakool et al.

Summary: Using the AlphaFold method, the structural coverage of the proteome has been significantly expanded, covering 98.5% of human proteins with 58% of residues having confident predictions and 36% having very high confidence. Introducing new metrics to interpret the dataset and identify disordered regions, this study aims to provide high-quality predictions for generating biological hypotheses.

NATURE (2021)

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Article Multidisciplinary Sciences

A nanobody activating metabotropic glutamate receptor 4 discriminates between homo-and heterodimers

Jordi Haubrich et al.

Summary: The article introduces a nanobody that can activate human mGlu4 homodimeric receptors and studies its effects on heterodimeric receptors. Through molecular modeling and mutagenesis studies, it reveals the mechanism of action of the nanobody.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

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Article Biochemistry & Molecular Biology

HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural studies of class IB phosphoinositide 3-kinases

Manoj K. Rathinaswamy et al.

Summary: This study successfully characterized multiple single-chain camelid nanobodies that bind to PI3K gamma using HDX mass spectrometry, revealing their ability to stimulate lipid kinase activity, block Ras activation, and specifically inhibit p101-mediated GPCR activation. These nanobodies provide insights into PI3K gamma regulation and potential therapeutic targets.

STRUCTURE (2021)

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Article Multidisciplinary Sciences

Structure, mechanism and crystallographic fragment screening of the SARS-CoV-2 NSP13 helicase

Joseph A. Newman et al.

Summary: The SARS-CoV-2 NSP13 helicase is crucial for viral replication and is considered a promising drug target. Crystal structures of NSP13 in different forms provide insights into its mechanism and potential inhibition methods. A crystallographic fragment screen identified 65 fragments bound to NSP13, offering opportunities for developing novel antiviral drugs.

NATURE COMMUNICATIONS (2021)

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Article Biology

Structure and analysis of nanobody binding to the human ASIC1a ion channel

Yangyu Wu et al.

Summary: The study demonstrates that nanobodies derived from alpacas specifically target human ASIC1a, offering potential therapeutic applications in modulating pain, fear, addiction, and ischemia-induced neuronal injury. In addition, the nanobody Nb.C1 can enhance inhibitory effects of tarantula toxin PcTx1 on hASIC1a and serve as a molecular tool for biochemical and structural studies of hASIC1a.

ELIFE (2021)

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Review Pharmacology & Pharmacy

An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters

Vojtech Dvorak et al.

Summary: The solute carrier (SLC) superfamily is the largest family of transporters with important roles in health and disease, yet many SLCs remain understudied. Challenges in SLC research include lack of tools for investigation and scattered information on assay strategies. The Innovative Medicines Initiative consortium RESOLUTE aims to accelerate research on SLCs by providing high-quality resources and data.

FRONTIERS IN PHARMACOLOGY (2021)

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Article Multidisciplinary Sciences

Achieving Efficient Fragment Screening at XChem Facility at Diamond Light Source

Alice Douangamath et al.

Summary: XChem technology is a facility for large-scale crystallographic fragment screening, which successfully transforms small molecules into potential drug candidates through intensive research efforts and improved techniques. This process has been widely applied to various therapeutic areas and has demonstrated flexibility and adaptability during the COVID-19 pandemic.

JOVE-JOURNAL OF VISUALIZED EXPERIMENTS (2021)

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Article Multidisciplinary Sciences

Cryo-EM structure of PepT2 reveals structural basis for proton-coupled peptide and prodrug transport in mammals

Joanne L. Parker et al.

Summary: The proton-coupled solute carriers PepT1 and PepT2 in the SLC15 family are crucial for acquiring dietary nitrogen and have extreme substrate promiscuity. Recent studies on their structure and function provide insights into their potential applications in drug development.

SCIENCE ADVANCES (2021)

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Article Biochemistry & Molecular Biology

ACE2-targeting monoclonal antibody as potent and broad-spectrum coronavirus blocker

Yuning Chen et al.

Summary: A monoclonal antibody called 3E8 was found to block multiple coronaviruses, including SARS-CoV-2 and its variants, without affecting the physiological activities of ACE2. It also showed effectiveness in blocking SARS-CoV-2 infection and provided a potential broad-spectrum strategy against coronaviruses that use ACE2 as entry receptors.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

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Review Biochemistry & Molecular Biology

Decoding the messaging of the ubiquitin system using chemical and protein probes

Lukas T. Henneberg et al.

Summary: Post-translational modification of proteins by ubiquitin is essential for eukaryotic cell function, with diverse targets and modifications acting as a complex communication system. Enzymatic assemblies like E1, E2, and E3 play messenger roles in modifying specific targets.

CELL CHEMICAL BIOLOGY (2021)

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Review Biochemistry & Molecular Biology

Ubiquitin ligases in cancer: Functions and clinical potentials

Shanshan Duan et al.

Summary: Ubiquitylation is a crucial post-translational modification that regulates many cellular pathways. Dysregulated ubiquitin ligases play critical roles in cancer initiation and progression, acting as either tumor promoters or tumor suppressors depending on substrates and contexts. Current research focuses on understanding the regulatory roles of ubiquitin ligases and developing strategies for cancer therapy.

CELL CHEMICAL BIOLOGY (2021)

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Article Biochemistry & Molecular Biology

DrugCentral 2021 supports drug discovery and repositioning

Sorin Avram et al.

Summary: DrugCentral is a public resource that offers up-to-date drug information, including newly approved drug ingredients, molecular entities related to COVID19, pharmacokinetic properties of drugs, sex-based separation of side effects, drug repositioning prioritization scheme, and machine learning platform for estimating anti-SARS-CoV-2 activities. Additionally, it provides a feature called 'drugs in news' for listing the most interesting drugs at the present moment.

NUCLEIC ACIDS RESEARCH (2021)

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Article Biochemistry & Molecular Biology

ProteomicsDB: a multi-omics and multi-organism resource for life science research

Patroklos Samaras et al.

NUCLEIC ACIDS RESEARCH (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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Article Biochemistry & Molecular Biology

Quantitative Proteomics of the Cancer Cell Line Encyclopedia

David P. Nusinow et al.

CELL (2020)

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Article Multidisciplinary Sciences

Structural basis for the recognition of SARS-CoV-2 by full-length human ACE2

Renhong Yan et al.

SCIENCE (2020)

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Editorial Material Chemistry, Medicinal

PROTAC Technology: Opportunities and Challenges

Hongying Gao et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

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Editorial Material Biotechnology & Applied Microbiology

The RESOLUTE consortium: unlocking SLC transporters for drug discovery

Giulio Superti-Furga et al.

NATURE REVIEWS DRUG DISCOVERY (2020)

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Article Biochemical Research Methods

FragMAX: the fragment-screening platform at the MAX IV Laboratory

Gustavo M. A. Lima et al.

ACTA CRYSTALLOGRAPHICA SECTION D-STRUCTURAL BIOLOGY (2020)

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Article Multidisciplinary Sciences

Synthetic nanobodies as angiotensin receptor blockers

Conor McMahon et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2020)

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Article Multidisciplinary Sciences

Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease

Alice Douangamath et al.

NATURE COMMUNICATIONS (2020)

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Article Biochemistry & Molecular Biology

Targeted Degradation of SLC Transporters Reveals Amenability of Multi-Pass Transmembrane Proteins to Ligand-Induced Proteolysis

Ariel Bensimon et al.

CELL CHEMICAL BIOLOGY (2020)

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Review Biochemistry & Molecular Biology

The role of ubiquitination in tumorigenesis and targeted drug discovery

Lu Deng et al.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2020)

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Review Biotechnology & Applied Microbiology

Applications of machine learning in drug discovery and development

Jessica Vamathevan et al.

NATURE REVIEWS DRUG DISCOVERY (2019)

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Article Biotechnology & Applied Microbiology

Deep learning enables rapid identification of potent DDR1 kinase inhibitors

Alex Zhavoronkov et al.

NATURE BIOTECHNOLOGY (2019)

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Article Chemistry, Analytical

Nanobody-based binding assay for the discovery of potent inhibitors of CFTR inhibitory factor (Cif)

Natalia Vasylieva et al.

ANALYTICA CHIMICA ACTA (2019)

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Article Biochemical Research Methods

UbiHub: a data hub for the explorers of ubiquitination pathways

Lihua Liu et al.

BIOINFORMATICS (2019)

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Article Biochemistry & Molecular Biology

ChEMBL: towards direct deposition of bioassay data

David Mendez et al.

NUCLEIC ACIDS RESEARCH (2019)

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Article Biochemical Research Methods

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology

Philip Brennecke et al.

SLAS DISCOVERY (2019)

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Review Biochemistry & Molecular Biology

From Discovery to Bedside: Targeting the Ubiquitin System

Ingrid E. Wertz et al.

CELL CHEMICAL BIOLOGY (2019)

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Review Cell Biology

The SLC transporter in nutrient and metabolic sensing, regulation, and drug development

Yong Zhang et al.

JOURNAL OF MOLECULAR CELL BIOLOGY (2019)

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Review Biochemistry & Molecular Biology

PROTACs: great opportunities for academia and industry

Xiuyun Sun et al.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2019)

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Article Chemistry, Medicinal

A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos

Mary E. Matyskiela et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

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Article Biochemistry & Molecular Biology

DrugBank 5.0: a major update to the DrugBank database for 2018

David S. Wishart et al.

NUCLEIC ACIDS RESEARCH (2018)

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Article Biochemistry & Molecular Biology

A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment

Marc L. Hyer et al.

NATURE MEDICINE (2018)

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Article Biology

Donated chemical probes for open science

Susanne Mueller et al.

ELIFE (2018)

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Article Pharmacology & Pharmacy

In silico Prioritization of Transporter-Drug Relationships From Drug Sensitivity Screens

Adrian Cesar-Razquin et al.

FRONTIERS IN PHARMACOLOGY (2018)

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Article Biochemistry & Molecular Biology

Objective, Quantitative, Data-Driven Assessment of Chemical Probes

Albert A. Antolin et al.

CELL CHEMICAL BIOLOGY (2018)

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Article Biotechnology & Applied Microbiology

A comprehensive map of molecular drug targets

Rita Santos et al.

NATURE REVIEWS DRUG DISCOVERY (2017)

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Letter Biochemical Research Methods

Probes & Drugs portal: an interactive, open data resource for chemical biology

Ctibor Skuta et al.

NATURE METHODS (2017)

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Article Biochemistry & Molecular Biology

Generation and Characterization of Anti-VGLUT Nanobodies Acting as Inhibitors of Transport

Stephan Schenck et al.

BIOCHEMISTRY (2017)

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Article Biochemistry & Molecular Biology

Defining a Cancer Dependency Map

Aviad Tsherniak et al.

CELL (2017)

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Article Oncology

Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology

Julian Blagg et al.

CANCER CELL (2017)

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Article Biochemistry & Molecular Biology

Correlating chemical sensitivity and basal gene expression reveals mechanism of action

Matthew G. Rees et al.

NATURE CHEMICAL BIOLOGY (2016)

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Article Multidisciplinary Sciences

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

Mary E. Matyskiela et al.

NATURE (2016)

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Article Biochemistry & Molecular Biology

Probes of ubiquitin E3 ligases enable systematic dissection of parkin activation

Kuan-Chuan Pao et al.

NATURE CHEMICAL BIOLOGY (2016)

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Article Cell Biology

Nanobodies that block gating of the P2X7 ion channel ameliorate inflammation

Welbeck Danquah et al.

SCIENCE TRANSLATIONAL MEDICINE (2016)

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Article Mathematical & Computational Biology

The harmonizome: a collection of processed datasets gathered to serve and mine knowledge about genes and proteins

Andrew D. Rouillard et al.

DATABASE-THE JOURNAL OF BIOLOGICAL DATABASES AND CURATION (2016)

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Article Hematology

CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL

Patrick R. Hagner et al.

BLOOD (2015)

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Review Biochemistry & Molecular Biology

A Call for Systematic Research on Solute Carriers

Adrian Cesar-Razquin et al.

CELL (2015)

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Review Biochemistry & Molecular Biology

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

Stuart L. Schreiber et al.

CELL (2015)

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Article Biochemistry & Molecular Biology

The promise and peril of chemical probes

Cheryl H. Arrowsmith et al.

NATURE CHEMICAL BIOLOGY (2015)

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Article Biochemical Research Methods

Assessment of a method to characterize antibody selectivity and specificity for use in immunoprecipitation

Edyta Marcon et al.

NATURE METHODS (2015)

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Article Biochemistry & Molecular Biology

ChEMBL web services: streamlining access to drug discovery data and utilities

Mark Davies et al.

NUCLEIC ACIDS RESEARCH (2015)

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Article Multidisciplinary Sciences

Tissue-based map of the human proteome

Mathias Uhlen et al.

SCIENCE (2015)

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Article Oncology

Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset

Brinton Seashore-Ludlow et al.

CANCER DISCOVERY (2015)

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Article Multidisciplinary Sciences

Nanobody-targeted E3-ubiquitin ligase complex degrades nuclear proteins

Yeong Ju Shin et al.

SCIENTIFIC REPORTS (2015)

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Article Biochemistry & Molecular Biology

DrugBank 4.0: shedding new light on drug metabolism

Vivian Law et al.

NUCLEIC ACIDS RESEARCH (2014)

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Article Biochemistry & Molecular Biology

An Interactive Resource to Identify Cancer Genetic and Lineage Dependencies Targeted by Small Molecules

Amrita Basu et al.

CELL (2013)

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Article Biochemistry & Molecular Biology

canSAR: an integrated cancer public translational research and drug discovery resource

Mark D. Halling-Brown et al.

NUCLEIC ACIDS RESEARCH (2012)

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Article Biochemistry & Molecular Biology

Pathway Commons, a web resource for biological pathway data

Ethan G. Cerami et al.

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