Small-Molecule Modulators for Epigenetics Targets

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

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

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

Strategy to Target the Substrate Binding site of SET Domain Protein Methyltransferases

(2013) Kong T. Nguyen et al.   Journal of Chemical Information and Modeling

Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors

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

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

(2013) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

The future of epigenetic therapy in solid tumours—lessons from the past

(2013) Nilofer Azad et al.   Nature Reviews Clinical Oncology

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

(2013) S. K. Knutson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

(2012) Guillermo Senisterra et al.   BIOCHEMICAL JOURNAL

ChromoHub: a data hub for navigators of chromatin-mediated signalling

(2012) L. Liu et al.   BIOINFORMATICS

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

(2012) Panagis Filippakopoulos et al.   CELL

Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

(2012) Aravind Basavapathruni et al.   Chemical Biology & Drug Design

Epigenetic Chemical Probes

(2012) S Müller et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

LSD1 inhibition: a therapeutic strategy in cancer?

(2012) James T Lynch et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor

(2012) Dominica Willmann et al.   INTERNATIONAL JOURNAL OF CANCER

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

(2012) Paul V. Fish et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stability of Nucleosomes Containing Homogenously Ubiquitylated H2A and H2B Prepared Using Semisynthesis

(2012) Beat Fierz et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Chromatin as an expansive canvas for chemical biology

(2012) Beat Fierz et al.   Nature Chemical Biology

Targeting genetic alterations in protein methyltransferases for personalized cancer therapeutics

(2012) R A Copeland et al.   ONCOGENE

An Allosteric Inhibitor of Protein Arginine Methyltransferase 3

(2012) Alena Siarheyeva et al.   STRUCTURE

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

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

Carbamate Prodrug Concept for Hydroxamate HDAC Inhibitors

(2011) Sonja Schlimme et al.   ChemMedChem

Structural Chemistry of the Histone Methyltransferases Cofactor Binding Site

(2011) Valérie Campagna-Slater et al.   Journal of Chemical Information and Modeling

Lysine Demethylases Inhibitors

(2011) Takayoshi Suzuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines

(2011) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 1: Inhibitor Binding Modes and Implications for Lead Discovery

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of Bromodomain Inhibitors Part 2: Optimization of Phenylisoxazole Sulfonamides

(2011) Paul Bamborough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Getting pharmaceutical R&D back on target

(2011) Mark E Bunnage   Nature Chemical Biology

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

(2011) Masoud Vedadi et al.   Nature Chemical Biology

The influence of the 'organizational factor' on compound quality in drug discovery

(2011) Paul D. Leeson et al.   NATURE REVIEWS DRUG DISCOVERY

Structural Basis of Substrate Methylation and Inhibition of SMYD2

(2011) Andrew D. Ferguson et al.   STRUCTURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Epigenetic modifications as therapeutic targets

(2010) Theresa K Kelly et al.   NATURE BIOTECHNOLOGY

Epigenetic modifications and human disease

(2010) Anna Portela et al.   NATURE BIOTECHNOLOGY

Epigenetic regulation of the neural transcriptome: the meaning of the marks

(2010) Michael J Meaney et al.   NATURE NEUROSCIENCE

Protein methyltransferases as a target class for drug discovery

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

Epigenetic control of plant stress response

(2007) Alex Boyko et al.   ENVIRONMENTAL AND MOLECULAR MUTAGENESIS