Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins

Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)

(2015) Harald Herrmann et al.   Oncotarget

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

(2014) Irfan A. Asangani et al.   NATURE

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

(2013) S. Picaud et al.   CANCER RESEARCH

Transcriptional/epigenetic regulator CBP/p300 in tumorigenesis: structural and functional versatility in target recognition

(2013) Feng Wang et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Target validation using chemical probes

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

Structure of the p300 catalytic core and implications for chromatin targeting and HAT regulation

(2013) Manuela Delvecchio et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

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

Discovery of BET bromodomain inhibitors and their role in target validation

(2013) S. Müller et al.   MedChemComm

From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151

(2012) Olivier Mirguet et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2012) Panagis Filippakopoulos et al.   CELL

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

The role of targeted chemical proteomics in pharmacology

(2011) Chris W Sutton   BRITISH JOURNAL OF PHARMACOLOGY

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

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

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

(2011) Mark A. Dawson et al.   NATURE

First drugs found to inhibit elusive cancer target

(2011) Melinda Wenner Moyer   NATURE MEDICINE

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Identifying the proteins to which small-molecule probes and drugs bind in cells

(2009) S.-E. Ong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Brd4 Coactivates Transcriptional Activation of NF- B via Specific Binding to Acetylated RelA

(2008) B. Huang et al.   MOLECULAR AND CELLULAR BIOLOGY