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 …

Bromodomain inhibitors and therapeutic applications

BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

A chemical toolbox for the study of bromodomains and epigenetic signaling

Q Wu, D Heidenreich, S Zhou, S Ackloo… - Nature …, 2019 - nature.com
Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …

Bromodomain drug discovery–the past, the present, and the future

M Pervaiz, P Mishra, S Günther - The Chemical Record, 2018 - Wiley Online Library
With the bromodomain (BRD) inhibitor JQ1, a remarkable success story of BRD4 as a novel
drug target has been set off that yielded many anti‐cancer drugs that are now in clinical …

Exploiting epigenetic targets to overcome taxane resistance in prostate cancer

B Cevatemre, I Bulut, B Dedeoglu, A Isiklar… - Cell Death & …, 2024 - nature.com
The development of taxane resistance remains a major challenge for castration resistant
prostate cancer (CR-PCa), despite the effectiveness of taxanes in prolonging patient …

Functional roles of bromodomain proteins in cancer

SP Boyson, C Gao, K Quinn, J Boyd, H Paculova… - Cancers, 2021 - mdpi.com
Simple Summary This review provides an in depth analysis of the role of bromodomain-
containing proteins in cancer development. As readers of acetylated lysine on nucleosomal …

Bone remodeling: histone modifications as fate determinants of bone cell differentiation

SJ Yi, H Lee, J Lee, K Lee, J Kim, Y Kim… - International journal of …, 2019 - mdpi.com
The bone tissue is a dynamic complex that constitutes of several interdependent systems
and is continuously remodeled through the concerted actions of bone cells. Osteoblasts are …

Bromodomain-containing protein BRPF1 is a therapeutic target for liver cancer

CLH Cheng, FHC Tsang, L Wei, M Chen… - Communications …, 2021 - nature.com
Epigenetic deregulation plays an essential role in hepatocellular carcinoma (HCC)
progression. Bromodomains are epigenetic “readers” of histone acetylation. Recently …

Selectively targeting individual bromodomain: Drug discovery and molecular mechanisms

Q Wang, X Shao, ELH Leung, Y Chen, X Yao - Pharmacological Research, 2021 - Elsevier
Bromodomain-containing proteins include bromodomain and extra-terminal (BET) and non-
BET families. Due to the conserved bromodomain (BD) module between BD-containing …

Bromodomain protein inhibition: a novel therapeutic strategy in rheumatic diseases

K Klein - RMD open, 2018 - rmdopen.bmj.com
The reading of acetylation marks on histones by bromodomain (BRD) proteins is a key event
in transcriptional activation. Small molecule inhibitors targeting bromodomain and extra …