Design and characterization of bivalent BET inhibitors

The Bromodomain: A New Target in Emerging Epigenetic Medicine

(2015) Steven G. Smith et al.   ACS Chemical Biology

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

PAINS in the Assay: Chemical Mechanisms of Assay Interference and Promiscuous Enzymatic Inhibition Observed during a Sulfhydryl-Scavenging HTS

(2015) Jayme L. Dahlin et al.   JOURNAL OF MEDICINAL CHEMISTRY

The promise and peril of chemical probes

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

A small-molecule inhibitor of the aberrant transcription factor CBF -SMMHC delays leukemia in mice

(2015) A. Illendula et al.   SCIENCE

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

The bromodomain: From epigenome reader to druggable target

(2014) Roberto Sanchez et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors

(2014) Michael R McKeown et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting bromodomains: epigenetic readers of lysine acetylation

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

A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

(2014) M. G. J. Baud et al.   SCIENCE

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

Genome-wide localization of small molecules

(2013) Lars Anders et al.   NATURE BIOTECHNOLOGY

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

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Exploiting structure similarity in refinement: automated NCS and target-structure restraints inBUSTER

(2012) Oliver S. Smart et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Small-Molecule Inhibition of BRDT for Male Contraception

(2012) Martin M. Matzuk et al.   CELL

Bromodomain and Extra-terminal (BET) Bromodomain Inhibition Activate Transcription via Transient Release of Positive Transcription Elongation Factor b (P-TEFb) from 7SK Small Nuclear Ribonucleoprotein

(2012) Koen Bartholomeeusen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition

(2012) Guangtao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A high-affinity, dimeric inhibitor of PSD-95 bivalently interacts with PDZ1-2 and protects against ischemic brain damage

(2012) A. Bach et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Two-pronged Binding with Bromodomain-containing Protein 4 Liberates Positive Transcription Elongation Factor b from Inactive Ribonucleoprotein Complexes

(2011) Sebastian Schröder et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

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

(2011) Mark A. Dawson et al.   NATURE

Integration, scaling, space-group assignment and post-refinement

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

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

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

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

The Mechanism of Release of P-TEFb and HEXIM1 from the 7SK snRNP by Viral and Cellular Activators Includes a Conformational Change in 7SK

(2010) Brian J. Krueger et al.   PLoS One

Design and Synthesis of Highly Potent and Plasma-Stable Dimeric Inhibitors of the PSD-95-NMDA Receptor Interaction

(2009) Anders Bach et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Expression and purification of recombinant annexin V for the detection of membrane alterations on apoptotic cells

(2008) Gabriela Brumatti et al.   METHODS