[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 …

Bromodomain biology and drug discovery

N Zaware, MM Zhou - Nature structural & molecular biology, 2019 - nature.com
The bromodomain (BrD) is a conserved structural module found in chromatin-and
transcription-associated proteins that acts as the primary reader for acetylated lysine …

Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …

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 …

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 …

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

S Picaud, C Wells, I Felletar… - Proceedings of the …, 2013 - National Acad Sciences
Bromodomains have emerged as attractive candidates for the development of inhibitors
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …

Chromatin proteins and modifications as drug targets

K Helin, D Dhanak - Nature, 2013 - nature.com
A plethora of groundbreaking studies have demonstrated the importance of chromatin-
associated proteins and post-translational modifications of histones, proteins and DNA (so …

BET bromodomains mediate transcriptional pause release in heart failure

P Anand, JD Brown, CY Lin, J Qi, R Zhang, PC Artero… - Cell, 2013 - cell.com
Heart failure (HF) is driven by the interplay between regulatory transcription factors and
dynamic alterations in chromatin structure. Pathologic gene transactivation in HF is …

The BET bromodomain inhibitor OTX015 affects pathogenetic pathways in preclinical B-cell tumor models and synergizes with targeted drugs

M Boi, E Gaudio, P Bonetti, I Kwee, E Bernasconi… - Clinical Cancer …, 2015 - AACR
Purpose: In cancer cells, the epigenome is often deregulated, and inhibition of the
bromodomain and extra-terminal (BET) family of bromodomain-containing proteins is a …