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 …

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

EJ Faivre, KF McDaniel, DH Albert, SR Mantena… - Nature, 2020 - nature.com
Proteins of the bromodomain and extra-terminal (BET) domain family are epigenetic readers
that bind acetylated histones through their bromodomains to regulate gene transcription …

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 …

The optimization of a novel, weak bromo and extra terminal domain (BET) bromodomain fragment ligand to a potent and selective second bromodomain (BD2) …

JT Seal, SJ Atkinson, H Aylott… - Journal of Medicinal …, 2020 - ACS Publications
The profound efficacy, yet associated toxicity of pan-BET inhibitors is well documented. The
possibility of an ameliorated safety profile driven by significantly selective (> 100-fold) …

Optimization of a series of 2, 3-dihydrobenzofurans as highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitors

SCC Lucas, SJ Atkinson, CW Chung… - Journal of Medicinal …, 2021 - ACS Publications
Herein, a series of 2, 3-dihydrobenzofurans have been developed as highly potent bromo
and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second …

Template-hopping approach leads to potent, selective, and highly soluble bromo and extraterminal domain (BET) second bromodomain (BD2) inhibitors

HE Aylott, SJ Atkinson, P Bamborough… - Journal of Medicinal …, 2021 - ACS Publications
A number of reports have recently been published describing the discovery and optimization
of bromo and extraterminal inhibitors which are selective for the second bromodomain …

Complementary, alternative and integrative medicine for childhood atopic dermatitis

KL Hon, AKC Leung, TNH Leung… - Recent Patents on …, 2017 - ingentaconnect.com
Background: Atopic Dermatitis (AD) is a chronic relapsing dermatosis associated with itch,
sleep disturbance and poor quality of life. Treatment of AD includes the use of emollients …

Enantio-and diastereoselective double Mannich reaction between ketones and imines catalyzed by Zn-prophenol

BM Trost, E Gnanamani - Organic letters, 2020 - ACS Publications
Herein we present a Zn-ProPhenol-catalyzed double Mannich reaction between ynones and
imines that generates 1, 3-diamines in excellent yield as well as diastereo-and …