Bromodomains: a new target class for drug development

AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

The functions of BET proteins in gene transcription of biology and diseases

KL Cheung, C Kim, MM Zhou - Frontiers in molecular biosciences, 2021 - frontiersin.org
The BET (bromodomain and extra-terminal domain) family proteins, consisting of BRD2,
BRD3, BRD4, and testis-specific BRDT, are widely acknowledged as major transcriptional …

Higher-order SPOP assembly reveals a basis for cancer mutant dysregulation

MJ Cuneo, BG O'Flynn, YH Lo, N Sabri, T Mittag - Molecular cell, 2023 - cell.com
The speckle-type POZ protein (SPOP) functions in the Cullin3-RING ubiquitin ligase (CRL3)
as a receptor for the recognition of substrates involved in cell growth, survival, and signaling …

Interactome rewiring following pharmacological targeting of BET bromodomains

JP Lambert, S Picaud, T Fujisawa, H Hou, P Savitsky… - Molecular cell, 2019 - cell.com
Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers
opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the …

Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases

E Kulikowski, BD Rakai… - Medicinal research …, 2021 - Wiley Online Library
Clinical development of bromodomain and extra‐terminal (BET) protein inhibitors differs
from the traditional course of drug development. These drugs are simultaneously being …

lncRNA DIGIT and BRD3 protein form phase-separated condensates to regulate endoderm differentiation

K Daneshvar, MB Ardehali, IA Klein, FK Hsieh… - Nature cell …, 2020 - nature.com
Cooperation between DNA, RNA and protein regulates gene expression and controls
differentiation through interactions that connect regions of nucleic acids and protein domains …

BET bromodomain inhibitors: novel design strategies and therapeutic applications

KKW To, E Xing, RC Larue, PK Li - Molecules, 2023 - mdpi.com
The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists
of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer …

Functional analysis of the replication fork proteome identifies BET proteins as PCNA regulators

SR Wessel, KN Mohni, JW Luzwick, H Dungrawala… - Cell reports, 2019 - cell.com
Identifying proteins that function at replication forks is essential to understanding DNA
replication, chromatin assembly, and replication-coupled DNA repair mechanisms …

Discovery of an MLLT1/3 YEATS domain chemical probe

M Moustakim, T Christott, OP Monteiro… - Angewandte Chemie …, 2018 - Wiley Online Library
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug
discovery. Dysregulation of these modified lysine‐binding proteins has been linked to the …

BRD4: a general regulator of transcription elongation

E Altendorfer, Y Mochalova, A Mayer - Transcription, 2022 - Taylor & Francis
Transcription elongation by RNA polymerase II (Pol II) has emerged as a regulatory hub in
gene expression. A key control point occurs during early transcription elongation when Pol II …