The polar warhead of a TRIM24 bromodomain inhibitor rearranges a water-mediated interaction network

Backbone resonance assignments for the PHD-Bromo dual-domain of the human chromatin reader TRIM24

(2016) Reto Walser et al.   Biomolecular NMR Assignments

TRIM24 Is an Oncogenic Transcriptional Activator in Prostate Cancer

(2016) Anna C. Groner et al.   CANCER CELL

NMR Fragment Screening Hit Induces Plasticity of BRD7/9 Bromodomains

(2016) Na Wang et al.   CHEMBIOCHEM

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

(2016) Terry D. Crawford et al.   JOURNAL OF MEDICINAL CHEMISTRY

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

(2015) Peter G. K. Clark et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fragment-Based Drug Discovery of 2-Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization

(2015) Lele Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF

(2015) James Bennett et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

(2015) Wylie S. Palmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Subset of Human Bromodomains Recognizes Butyryllysine and Crotonyllysine Histone Peptide Modifications

(2015) E. Megan Flynn et al.   STRUCTURE

TRIM24 is upregulated in human gastric cancer and promotes gastric cancer cell growth and chemoresistance

(2015) Zhi-Feng Miao et al.   VIRCHOWS ARCHIV

Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer

(2014) Irfan A. Asangani et al.   NATURE

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

TRIM24 promotes glioma progression and enhances chemoresistance through activation of the PI3K/Akt signaling pathway

(2014) L-H Zhang et al.   ONCOGENE

Knockdown of Tripartite Motif Containing 24 by Lentivirus Suppresses Cell Growth and Induces Apoptosis in Human Colorectal Cancer Cells

(2014) Jianwei Wang et al.   ONCOLOGY RESEARCH

Overexpression of TRIM24 Is Associated with the Onset and Progress of Human Hepatocellular Carcinoma

(2014) Xiao Liu et al.   PLoS One

Automated NMR Fragment Based Screening Identified a Novel Interface Blocker to the LARG/RhoA Complex

(2014) Jia Gao et al.   PLoS One

Ubiquitylome analysis identifies dysregulation of effector substrates in SPOP-mutant prostate cancer

(2014) J.-P. P. Theurillat et al.   SCIENCE

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

(2014) Emmanuel H. Demont et al.   ACS Medicinal Chemistry Letters

BET Bromodomains Mediate Transcriptional Pause Release in Heart Failure

(2013) Priti Anand et al.   CELL

TRIM24 Overexpression Is Common in Locally Advanced Head and Neck Squamous Cell Carcinoma and Correlates with Aggressive Malignant Phenotypes

(2013) Zhibin Cui et al.   PLoS One

Using chemical shift perturbation to characterise ligand binding

(2013) Mike P. Williamson   PROGRESS IN NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY

Small-Molecule Inhibition of BRDT for Male Contraception

(2012) Martin M. Matzuk et al.   CELL

Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions

(2012) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

Epigenetic protein families: a new frontier for drug discovery

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

Overexpression of TRIM24 Correlates with Tumor Progression in Non-Small Cell Lung Cancer

(2012) Haiying Li et al.   PLoS One

Prognostic Significance of TRIM24/TIF-1α Gene Expression in Breast Cancer

(2011) Monique Chambon et al.   AMERICAN JOURNAL OF PATHOLOGY

Saturation-Transfer Difference (STD) NMR: A Simple and Fast Method for Ligand Screening and Characterization of Protein Binding

(2011) Aldino Viegas et al.   JOURNAL OF CHEMICAL EDUCATION

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

TRIM24 links a non-canonical histone signature to breast cancer

(2010) Wen-Wei Tsai et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Molecular replacement withMOLREP

(2009) Alexei Vagin et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Trim24 targets endogenous p53 for degradation

(2009) Kendra Allton et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA