Recent progress and structural analyses of domain‐selective BET inhibitors

A Divakaran, DA Harki… - Medicinal research …, 2023 - Wiley Online Library
Epigenetic mechanisms for controlling gene expression through heritable modifications to
DNA, RNA, and proteins, are essential processes in maintaining cellular homeostasis. As a …

Small molecule inhibitors of bromodomain–acetyl-lysine interactions

M Brand, AM Measures, BG Wilson… - ACS chemical …, 2015 - ACS Publications
Bromodomains are protein modules that bind to acetylated lysine residues. Their interaction
with histone proteins suggests that they function as “readers” of histone lysine acetylation, a …

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

A Hammitzsch, C Tallant, O Fedorov… - Proceedings of the …, 2015 - pnas.org
Th17 responses are critical to a variety of human autoimmune diseases, and therapeutic
targeting with monoclonal antibodies against IL-17 and IL-23 has shown considerable …

The SMARCA2/4 ATPase domain surpasses the bromodomain as a drug target in SWI/SNF-mutant cancers: insights from cDNA rescue and PFI-3 inhibitor studies

B Vangamudi, TA Paul, PK Shah, M Kost-Alimova… - Cancer …, 2015 - aacrjournals.org
The SWI/SNF multisubunit complex modulates chromatin structure through the activity of two
mutually exclusive catalytic subunits, SMARCA2 and SMARCA4, which both contain a …

Structure-based design of an in vivo active selective BRD9 inhibitor

LJ Martin, M Koegl, G Bader, XL Cockcroft… - Journal of medicinal …, 2016 - ACS Publications
Components of the chromatin remodelling switch/sucrose nonfermentable (SWI/SNF)
complex are recurrently mutated in tumors, suggesting that altering the activity of the …

Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy

S Picaud, O Fedorov, A Thanasopoulou… - Cancer …, 2015 - aacrjournals.org
The histone acetyltransferases CBP/p300 are involved in recurrent leukemia-associated
chromosomal translocations and are key regulators of cell growth. Therefore, efforts to …

LP99: discovery and synthesis of the first selective BRD7/9 bromodomain inhibitor

PGK Clark, LCC Vieira, C Tallant… - Angewandte …, 2015 - Wiley Online Library
The bromodomain‐containing proteins BRD9 and BRD7 are part of the human SWI/SNF
chromatin‐remodeling complexes BAF and PBAF. To date, no selective inhibitor for BRD7/9 …

Disrupting acetyl-lysine recognition: progress in the development of bromodomain inhibitors

FA Romero, AM Taylor, TD Crawford… - Journal of medicinal …, 2016 - ACS Publications
Bromodomains, small protein modules that recognize acetylated lysine on histones, play a
significant role in the epigenome, where they function as “readers” that ultimately determine …

Potent and selective bivalent inhibitors of BET bromodomains

MJ Waring, H Chen, AA Rabow, G Walker… - Nature chemical …, 2016 - nature.com
Proteins of the bromodomain and extraterminal (BET) family, in particular bromodomain-
containing protein 4 (BRD4), are of great interest as biological targets. BET proteins contain …

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

O Fedorov, J Castex, C Tallant, DR Owen, S Martin… - Science …, 2015 - science.org
Mammalian SWI/SNF [also called Brg/Brahma-associated factors (BAFs)] are evolutionarily
conserved chromatin-remodeling complexes regulating gene transcription programs during …