4.7 Article

Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1

Related references

Note: Only part of the references are listed.
Article Chemistry, Medicinal

Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1

Dongxing Chen et al.

Summary: Protein N-terminal methyltransferases (NTMTs) play a role in cancer and aging, making them potential therapeutic targets. By modifying a lead NTMT1 inhibitor, researchers created a more potent inhibitor, DC541, with increased activity and over 300-fold selectivity to other methyltransferases. This study provides a direction for the development of more cell-potent inhibitors for NTMT1.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

News Item Biotechnology & Applied Microbiology

Targeted protein degraders crowd into the clinic

Asher Mullard

NATURE REVIEWS DRUG DISCOVERY (2021)

Review Chemistry, Multidisciplinary

From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation

Carlotta Cecchini et al.

Summary: PROTACs are heterobifunctional degraders that eliminate targeted proteins by utilizing the UPS system, showing potential as an appealing technology in drug discovery. However, their poor cellular permeability due to high molecular weight and large polar surface area poses challenges, requiring strategies and biological tools to enhance cellular uptake.

FRONTIERS IN CHEMISTRY (2021)

Review Biochemistry & Molecular Biology

Past, present, and perspectives of protein N-terminal methylation

Krystal Diaz et al.

Summary: The posttranslational methylation of the alpha-N-terminal amino group of proteins, first documented over 40 years ago, has been relatively less explored compared to lysine and arginine methylation. Increasing reports suggest that alpha-N-terminal methylation plays a widespread and critical regulatory role in mitosis, chromatin interactions, DNA repair, and translation fidelity. Recent advances include the understanding of biological functions and mechanisms, substrate recognition, discovery of inhibitors, and crosstalk with other N-terminal modifications.

CURRENT OPINION IN CHEMICAL BIOLOGY (2021)

Review Chemistry, Multidisciplinary

E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points

Alesa Bricelj et al.

Summary: PROTACs, as a new and exciting class of therapeutic agents, consist of target binding units, linkers, and E3 ligase binding moieties, leading to ubiquitination and proteasomal degradation of target proteins through the chemically-induced formation of ternary complexes. This review provides in-depth analysis on the synthetic preparation of functionalized ligands for relevant E3 ligases, highlighting the importance of understanding preparative routes and chemistry of linker attachment for the assembly of final PROTACs.

FRONTIERS IN CHEMISTRY (2021)

Review Biochemistry & Molecular Biology

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

Michael J. Bond et al.

Summary: The discovery of PROTACs has revolutionized targeted protein degradation, leading to the development of orally bioavailable clinical drugs. Future advancements in technology will expedite the discovery of new degraders and E3 ligases, as well as the identification of active degraders.

RSC CHEMICAL BIOLOGY (2021)

Review Cell Biology

Calreticulin and cancer

Jitka Fucikova et al.

Summary: CALR is a protein located in the endoplasmic reticulum that plays important roles in cellular processes and protein folding. It acts as a chaperone in healthy cells, assisting protein folding and supporting Ca2+-dependent processes, while also being exposed on the cell surface in cancer cells to promote immunogenic cell death. Loss-of-functionCALRmutations can promote oncogenesis by impairing cellular homeostasis and compromising natural and therapy-driven immunosurveillance.

CELL RESEARCH (2021)

Review Biochemistry & Molecular Biology

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

George M. Burslem et al.

Article Chemistry, Organic

A Facile Synthesis of Ligands for the von Hippel-Lindau E3 Ligase

Christian Steinebach et al.

SYNTHESIS-STUTTGART (2020)

Article Chemistry, Medicinal

Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues

Dongxing Chen et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Medicinal

Understanding and Improving the Membrane Permeability of VH032-Based PROTACs

Victoria G. Klein et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

Review Cell Biology

Detection of immunogenic cell death and its relevance for cancer therapy

Jitka Fucikova et al.

CELL DEATH & DISEASE (2020)

Review Biochemistry & Molecular Biology

Is It Time to Start Transitioning From 2D to 3D Cell Culture?

Caleb Jensen et al.

FRONTIERS IN MOLECULAR BIOSCIENCES (2020)

Article Chemistry, Medicinal

Discovery of Bisubstrate Inhibitors for Protein N-Terminal Methyltransferase 1

Dongxing Chen et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

Carl C. Ward et al.

ACS CHEMICAL BIOLOGY (2019)

Review Biochemistry & Molecular Biology

Calreticulin in phagocytosis and cancer: opposite roles in immune response outcomes

Alejandro Schcolnik-Cabrera et al.

APOPTOSIS (2019)

Article Chemistry, Medicinal

Dual-targeting Rutaecarpine-NO donor hybrids as novel anti-hypertensive agents by promoting release of CGRP

Jinjin Ma et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Medicine, Research & Experimental

BETP degradation simultaneously targets acute myelogenous leukemic stem cells and the microenvironment

Sujan Piya et al.

JOURNAL OF CLINICAL INVESTIGATION (2019)

Review Biochemistry & Molecular Biology

Advances in targeted degradation of endogenous proteins

Sascha Roth et al.

CELLULAR AND MOLECULAR LIFE SCIENCES (2019)

Article Biochemistry & Molecular Biology

Calreticulin is a Critical Cell Survival Factor in Malignant Neoplasms

Arum Han et al.

PLOS BIOLOGY (2019)

Article Multidisciplinary Sciences

3D cell culture stimulates the secretion of in vivo like extracellular vesicles

Sirisha Thippabhotla et al.

SCIENTIFIC REPORTS (2019)

Review Biochemistry & Molecular Biology

Chemical Biology of Protein N-Terminal Methyltransferases

Rong Huang

CHEMBIOCHEM (2019)

Article Chemistry, Multidisciplinary

In vivo methylation of OLA1 revealed by activity-based target profiling of NTMT1

Kaimin Jia et al.

CHEMICAL SCIENCE (2019)

Review Gastroenterology & Hepatology

Epidemiology of colorectal cancer: incidence, mortality, survival, and risk factors

Prashanth Rawla et al.

GASTROENTEROLOGY REVIEW-PRZEGLAD GASTROENTEROLOGICZNY (2019)

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)

Review Biochemistry & Molecular Biology

The ribosome: A hot spot for the identification of new types of protein methyltransferases

Steven G. Clarke

JOURNAL OF BIOLOGICAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Lara N. Gechijian et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

N-terminal acetylation and methylation differentially affect the function of MYL9

Chris Nevitt et al.

BIOCHEMICAL JOURNAL (2018)

Review Oncology

Trial watch: Peptide-based vaccines in anticancer therapy

Lucillia Bezu et al.

ONCOIMMUNOLOGY (2018)

Article Chemistry, Multidisciplinary

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

George M. Burslem et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2018)

Article Biochemistry & Molecular Biology

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Daniel P. Bondeson et al.

CELL CHEMICAL BIOLOGY (2018)

Article Biochemistry & Molecular Biology

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

George M. Burslem et al.

CELL CHEMICAL BIOLOGY (2018)

Review Biotechnology & Applied Microbiology

Induced protein degradation: an emerging drug discovery paradigm

Ashton C. Lai et al.

NATURE REVIEWS DRUG DISCOVERY (2017)

Article Biochemistry & Molecular Biology

Structural basis of PROTAC cooperative recognition for selective protein degradation

Morgan S. Gadd et al.

NATURE CHEMICAL BIOLOGY (2017)

Article Biochemistry & Molecular Biology

Select human cancer mutants of NRMT1 alter its catalytic activity and decrease N-terminal trimethylation

Kaitlyn M. Shields et al.

PROTEIN SCIENCE (2017)

Article Multidisciplinary Sciences

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Kanak Raina et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2016)

Article Multidisciplinary Sciences

Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

Julianty Frost et al.

NATURE COMMUNICATIONS (2016)

Article Biochemistry & Molecular Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Jing Lu et al.

CHEMISTRY & BIOLOGY (2015)

Article Cell Biology

Molecular basis for histone N-terminal methylation by NRMT1

Ruoxi Wu et al.

GENES & DEVELOPMENT (2015)

Article Cell Biology

NRMT1 knockout mice exhibit phenotypes associated with impaired DNA repair and premature aging

Lindsay A. Bonsignore et al.

MECHANISMS OF AGEING AND DEVELOPMENT (2015)

Article Biochemistry & Molecular Biology

Catalytic in vivo protein knockdown by small-molecule PROTACs

Daniel P. Bondeson et al.

NATURE CHEMICAL BIOLOGY (2015)

Article Chemistry, Organic

Design, synthesis, and kinetic analysis of potent protein N-terminal methyltransferase 1 inhibitors

Gang Zhang et al.

ORGANIC & BIOMOLECULAR CHEMISTRY (2015)

Article Multidisciplinary Sciences

Phthalimide conjugation as a strategy for in vivo target protein degradation

Georg E. Winter et al.

SCIENCE (2015)

Article Biochemistry & Molecular Biology

α-N-Methylation of Damaged DNA-binding Protein 2 (DDB2) and Its Function in Nucleotide Excision Repair

Qian Cai et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2014)

Article Biochemistry & Molecular Biology

NRMT2 is an N-terminal monomethylase that primes for its homologue NRMT1

Janusz J. Petkowski et al.

BIOCHEMICAL JOURNAL (2013)

Article Biochemical Research Methods

Identification of Novel α-N-Methylation of CENP-B That Regulates Its Binding to the Centromeric DNA

Xiaoxia Dai et al.

JOURNAL OF PROTEOME RESEARCH (2013)

Article Multidisciplinary Sciences

Posttranslational modification of CENP-A influences the conformation of centromeric chromatin

Aaron O. Bailey et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2013)

Article Biochemistry & Molecular Biology

Identification of Protein N-Terminal Methyltransferases in Yeast and Humans

Kristofor J. Webb et al.

BIOCHEMISTRY (2010)

Article Biochemistry & Molecular Biology

RCC1 Uses a Conformationally Diverse Loop Region to Interact with the Nucleosome: A Model for the RCC1-Nucleosome Complex

Joseph R. England et al.

JOURNAL OF MOLECULAR BIOLOGY (2010)

Article Multidisciplinary Sciences

NRMT is an α-N-methyltransferase that methylates RCC1 and retinoblastoma protein

Christine E. Schaner Tooley et al.

NATURE (2010)

Article Gastroenterology & Hepatology

Expression of calreticulin is associated with infiltration of T-cells in stage III B colon cancer

Rui-Qing Peng et al.

WORLD JOURNAL OF GASTROENTEROLOGY (2010)

Review Cell & Tissue Engineering

Three-dimensional cell culture matrices: State of the art

Jungwoo Lee et al.

TISSUE ENGINEERING PART B-REVIEWS (2008)

Article Oncology

Transcriptome profile of human colorectal adenomas

Jacob Sabates-Beliver et al.

MOLECULAR CANCER RESEARCH (2007)