[HTML][HTML] 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 …

Lysine acetylation goes global: from epigenetics to metabolism and therapeutics

I Ali, RJ Conrad, E Verdin, M Ott - Chemical reviews, 2018 - ACS Publications
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …

Clinical response of carcinomas harboring the BRD4–NUT oncoprotein to the targeted bromodomain inhibitor OTX015/MK-8628

A Stathis, E Zucca, M Bekradda, C Gomez-Roca… - Cancer discovery, 2016 - AACR
The antineoplastic, prodifferentiative effects of bromodomain and extra-terminal (BET)
bromodomain (BRD) inhibitors were initially discovered in NUT midline carcinoma (NMC) …

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 - Future Science
Histone lysine acetylation is critical in regulating transcription. Dysregulation of this process
results in aberrant gene expression in various diseases, including cancer. The …

Marked for death: targeting epigenetic changes in cancer

SX Pfister, A Ashworth - Nature reviews Drug discovery, 2017 - nature.com
In the past few years, it has become clear that mutations in epigenetic regulatory genes are
common in human cancers. Therapeutic strategies are now being developed to target …

Phase 1 study of molibresib (GSK525762), a bromodomain and extra-terminal domain protein inhibitor, in NUT carcinoma and other solid tumors

SA Piha-Paul, CL Hann, CA French… - JNCI Cancer …, 2020 - academic.oup.com
Background Bromodomain and extra-terminal domain proteins are promising epigenetic
anticancer drug targets. This first-in-human study evaluated the safety, recommended phase …

An anatomical site and genetic-based prognostic model for patients with nuclear protein in testis (NUT) midline carcinoma: analysis of 124 patients

NG Chau, C Ma, K Danga, H Al-Sayegh… - JNCI Cancer …, 2020 - academic.oup.com
Background NUT midline carcinoma, renamed NUT carcinoma (NC), is an aggressive
squamous cancer defined by rearrangement of the NUTM1 gene. Although a subset of …

[HTML][HTML] BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells

MM Coudé, T Braun, J Berrou, M Dupont, S Bertrand… - Oncotarget, 2015 - ncbi.nlm.nih.gov
The bromodomain (BRD) and extraterminal (BET) proteins including BRD2, BRD3 and
BRD4 have been identified as key targets for leukemia maintenance. A novel oral inhibitor of …

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 …

NUT Carcinoma: Clinicopathologic features, pathogenesis, and treatment

CA French - Pathology international, 2018 - Wiley Online Library
NUT carcinoma (NC) is a rare, aggressive subtype of squamous cell carcinoma defined by
rearrangement of the NUTM1 (aka NUT) gene. NC is driven by NUT‐fusion oncoproteins …