Achieving clinical success with BET inhibitors as anti-cancer agents

T Shorstova, WD Foulkes, M Witcher - British journal of cancer, 2021 - nature.com
The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …

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 …

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 …

BET proteins as targets for anticancer treatment

A Stathis, F Bertoni - Cancer discovery, 2018 - AACR
Bromodomain and extraterminal domain (BET) proteins are epigenetic readers that regulate
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …

Bromodomain and extra-terminal motif inhibitors: a review of preclinical and clinical advances in cancer therapy

A Alqahtani, K Choucair, M Ashraf… - Future science …, 2019 - Taylor & Francis
Histone lysine acetylation is critical in regulating transcription. Dysregulation of this process
results in aberrant gene expression in various diseases, including cancer. The …

Drug resistance to targeted therapeutic strategies in non-small cell lung cancer

W Liu, Y Du, R Wen, M Yang, J Xu - Pharmacology & therapeutics, 2020 - Elsevier
Rapidly developing molecular biology techniques have been employed to identify cancer
driver genes in specimens from patients with non-small cell lung cancer (NSCLC). Inhibitors …

Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction

M Yin, Y Guo, R Hu, WL Cai, Y Li, S Pei, H Sun… - Nature …, 2020 - nature.com
Small molecule inhibitor of the bromodomain and extraterminal domain (BET) family
proteins is a promising option for cancer treatment. However, current BET inhibitors are …

Targeting the Bcl-2 family in B cell lymphoma

CM Adams, S Clark-Garvey, P Porcu… - Frontiers in …, 2019 - frontiersin.org
Although lymphoma is a very heterogeneous group of biologically complex malignancies,
tumor cells across all B cell lymphoma subtypes share a set of underlying traits that promote …

First-in-human study of mivebresib (ABBV-075), an oral pan-inhibitor of bromodomain and extra terminal proteins, in patients with relapsed/refractory solid tumors

SA Piha-Paul, JC Sachdev, M Barve, P LoRusso… - Clinical Cancer …, 2019 - AACR
Purpose: Bromodomain and extraterminal (BET) proteins play important roles in
transcriptional regulation relevant to cancer pathogenesis, and therapeutic …

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 …