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 …

Epigenetics in cancer stem cells

TB Toh, JJ Lim, EKH Chow - Molecular cancer, 2017 - Springer
Compelling evidence have demonstrated that bulk tumors can arise from a unique subset of
cells commonly termed “cancer stem cells” that has been proposed to be a strong driving …

[HTML][HTML] BET inhibitors: a novel epigenetic approach

DB Doroshow, JP Eder, PM LoRusso - Annals of Oncology, 2017 - Elsevier
Epigenetics has been defined as 'the structural adaptation of chromosomal regions so as to
register, signal or perpetuate altered activity states.'Currently, several classes of anticancer …

Targeting bromodomains: epigenetic readers of lysine acetylation

P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …

Discovery of a small-molecule degrader of bromodomain and extra-terminal (BET) proteins with picomolar cellular potencies and capable of achieving tumor …

B Zhou, J Hu, F Xu, Z Chen, L Bai… - Journal of medicinal …, 2018 - ACS Publications
The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3,
BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in …

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 …

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 …

Bromodomain inhibitors and cancer therapy: From structures to applications

M Pérez-Salvia, M Esteller - Epigenetics, 2017 - Taylor & Francis
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes
that are “writers,”“erasers,” or “readers” of histone modification marks are common …

An update of epigenetic drugs for the treatment of cancers and brain diseases: a comprehensive review

Z Sahafnejad, S Ramazi, A Allahverdi - Genes, 2023 - mdpi.com
Epigenetics has long been recognized as a significant field in biology and is defined as the
investigation of any alteration in gene expression patterns that is not attributed to changes in …

Targeting epigenetics in cancer

RL Bennett, JD Licht - Annual review of pharmacology and …, 2018 - annualreviews.org
Alterations of genes regulating epigenetic processes are frequently found as cancer drivers
and may cause widespread alterations of DNA methylation, histone modification patterns, or …