Discovery of a PCAF Bromodomain Chemical Probe

A Chemical Probe for the ATAD2 Bromodomain

(2016) Paul Bamborough et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Progress in the Development of non-BET Bromodomain Chemical Probes

(2016) Natalie H. Theodoulou et al.   ChemMedChem

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain

(2016) Apirat Chaikuad et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

(2016) Charlotte L. Sutherell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

(2016) Laetitia J. Martin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

(2016) Brian S. Gerstenberger et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

(2016) Oakley B. Cox et al.   Chemical Science

Chemical probes and inhibitors of bromodomains outside the BET family

(2016) Moses Moustakim et al.   MedChemComm

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

(2016) Paul Bamborough et al.   ACS Medicinal Chemistry Letters

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia

(2016) S. Picaud et al.   Science Advances

NanoBRET—A Novel BRET Platform for the Analysis of Protein–Protein Interactions

(2015) Thomas Machleidt et al.   ACS Chemical Biology

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B

(2015) Peiling Chen 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

Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain

(2015) Andrea Unzue et al.   JOURNAL OF MEDICINAL CHEMISTRY

The promise and peril of chemical probes

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

Fluorescence Polarization for the Evaluation of Small-Molecule Inhibitors of PCAF BRD/Tat-AcK50 Association

(2014) Ping Hu et al.   ChemMedChem

Targeting bromodomains: epigenetic readers of lysine acetylation

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

Lysine Acetyltransferase PCAF Is a Key Regulator of Arteriogenesis

(2013) Antonius J.N.M. Bastiaansen et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

BET bromodomain inhibitors: a patent review

(2013) Jean-Marc Garnier et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains

(2013) Oleg Fedorov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication

(2013) Qiang Wang et al.   MedChemComm

Docking and scoring with ICM: the benchmarking results and strategies for improvement

(2012) Marco A. C. Neves et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites

(2012) Lewis R. Vidler 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

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE