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Recent progress and structural analyses of domain‐selective BET inhibitors
Epigenetic mechanisms for controlling gene expression through heritable modifications to
DNA, RNA, and proteins, are essential processes in maintaining cellular homeostasis. As a …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
significant role in the epigenome, where they function as “readers” that ultimately determine …
Potent and selective bivalent inhibitors of BET bromodomains
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 …
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 …
conserved chromatin-remodeling complexes regulating gene transcription programs during …