A chemical biology toolbox to study protein methyltransferases and epigenetic signaling

Loss of Eed leads to lineage instability and increased CD8 expression of mouse CD4 + T cells upon TGFβ signaling

(2018) Taku Naito et al.   MOLECULAR IMMUNOLOGY

The epigenetic control of stemness in CD8+T cell fate commitment

(2018) Luigia Pace et al.   SCIENCE

Beyond histones - the expanding roles of protein lysine methylation

(2017) Zhouran Wu et al.   FEBS Journal

Methylarginines within the RGG-Motif Region of hnRNP A1 Affect Its IRES Trans -Acting Factor Activity and Are Required for hnRNP A1 Stress Granule Localization and Formation

(2017) Michael L. Wall et al.   JOURNAL OF MOLECULAR BIOLOGY

Loss of Protein Arginine Methyltransferase 8 Alters Synapse Composition and Function, Resulting in Behavioral Defects

(2017) Jay Penney et al.   JOURNAL OF NEUROSCIENCE

An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED

(2017) Wei Qi et al.   Nature Chemical Biology

The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex

(2017) Yupeng He et al.   Nature Chemical Biology

The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity

(2017) Kenneth D Bromberg et al.   Nature Chemical Biology

Targeted protein degradation by PROTACs

(2017) Taavi K. Neklesa et al.   PHARMACOLOGY & THERAPEUTICS

Structural Basis for Substrate Preference of SMYD3, a SET Domain-containing Protein Lysine Methyltransferase

(2016) Weiqi Fu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6

(2016) Yudao Shen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2

(2016) Erik Eggert et al.   JOURNAL OF MEDICINAL CHEMISTRY

Functional interdependence of BRD4 and DOT1L in MLL leukemia

(2016) Omer Gilan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

(2016) Alexei Brooun et al.   Nature Communications

Functional interdependence of BRD4 and DOT1L in MLL leukemia

(2016) Omer Gilan et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases

(2015) Mohammad S. Eram et al.   ACS Chemical Biology

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

(2015) H. Ümit Kaniskan et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

(2015) Florian Grebien et al.   Nature Chemical Biology

The promise and peril of chemical probes

(2015) Cheryl H Arrowsmith et al.   Nature Chemical Biology

2016 update of the PRIDE database and its related tools

(2015) Juan Antonio Vizcaíno et al.   NUCLEIC ACIDS RESEARCH

Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666

(2015) Kenneth W. Duncan et al.   ACS Medicinal Chemistry Letters

The polycomb repressive complex 2 governs life and death of peripheral T cells

(2014) Y. Zhang et al.   BLOOD

Methyltransferase G9A regulates T cell differentiation during murine intestinal inflammation

(2014) Frann Antignano et al.   JOURNAL OF CLINICAL INVESTIGATION

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

(2014) D. Barsyte-Lovejoy et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

(2014) Ramzi F. Sweis et al.   ACS Medicinal Chemistry Letters

An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1

(2013) Kyle D. Konze et al.   ACS Chemical Biology

The Polycomb Protein Ezh2 Regulates Differentiation and Plasticity of CD4+ T Helper Type 1 and Type 2 Cells

(2013) Damon J. Tumes et al.   IMMUNITY

Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP

(2013) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Locus-specific editing of histone modifications at endogenous enhancers

(2013) Eric M Mendenhall et al.   NATURE BIOTECHNOLOGY

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Regulation of estrogen receptor   by histone methyltransferase SMYD2-mediated protein methylation

(2013) X. Zhang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein arginine methyltransferase 5 is a potential oncoprotein that upregulates G1 cyclins/cyclin-dependent kinases and the phosphoinositide 3-kinase/AKT signaling cascade

(2012) Tong-You W. Wei et al.   CANCER SCIENCE

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

(2012) Michael T. McCabe et al.   NATURE

Epigenetic protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

(2012) Sharad K. Verma et al.   ACS Medicinal Chemistry Letters

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Methylation of Ribosomal Protein S10 by Protein-arginine Methyltransferase 5 Regulates Ribosome Biogenesis

(2010) Jinqi Ren et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Activating and inhibitory functions for the histone lysine methyltransferase G9a in T helper cell differentiation and function

(2010) Bernhard Lehnertz et al.   JOURNAL OF EXPERIMENTAL MEDICINE

The art of the chemical probe

(2010) Stephen V Frye   Nature Chemical Biology

Mechanisms Underlying Lineage Commitment and Plasticity of Helper CD4+ T Cells

(2010) J. J. O'Shea et al.   SCIENCE

Kinetic analysis of human protein arginine N-methyltransferase 2: formation of monomethyl- and asymmetric dimethyl-arginine residues on histone H4

(2009) Ted M. Lakowski et al.   BIOCHEMICAL JOURNAL

Cytokine-secreting follicular T cells shape the antibody repertoire

(2009) R Lee Reinhardt et al.   NATURE IMMUNOLOGY

Protein methyltransferases as a target class for drug discovery

(2009) Robert A. Copeland et al.   NATURE REVIEWS DRUG DISCOVERY

PRMT5 is required for cell-cycle progression and p53 tumor suppressor function

(2009) A. Scoumanne et al.   NUCLEIC ACIDS RESEARCH

CD4 T cells: fates, functions, and faults

(2008) J. Zhu et al.   BLOOD