[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 …

Epigenetic therapies for cancer

SE Bates - New England Journal of Medicine, 2020 - Mass Medical Soc
Epigenetic Therapies for Cancer | New England Journal of Medicine Skip to main content The
New England Journal of Medicine homepage Advanced Search SEARCH SPECIALTIES …

Combining epigenetic drugs with other therapies for solid tumours—past lessons and future promise

D Morel, D Jeffery, S Aspeslagh, G Almouzni… - Nature Reviews …, 2020 - nature.com
Epigenetic dysregulation has long been recognized as a key factor contributing to
tumorigenesis and tumour maintenance that can influence all of the recognized hallmarks of …

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 …

[HTML][HTML] A phase separation model for transcriptional control

D Hnisz, K Shrinivas, RA Young, AK Chakraborty… - Cell, 2017 - cell.com
Phase-separated multi-molecular assemblies provide a general regulatory mechanism to
compartmentalize biochemical reactions within cells. We propose that a phase separation …

[HTML][HTML] Transcriptional addiction in cancer

JE Bradner, D Hnisz, RA Young - Cell, 2017 - cell.com
Cancer arises from genetic alterations that invariably lead to dysregulated transcriptional
programs. These dysregulated programs can cause cancer cells to become highly …

Plasticity in binding confers selectivity in ligand-induced protein degradation

RP Nowak, SL DeAngelo, D Buckley, Z He… - Nature chemical …, 2018 - nature.com
Heterobifunctional small-molecule degraders that induce protein degradation through ligase-
mediated ubiquitination have shown considerable promise as a new pharmacological …

Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

HP Mohammad, O Barbash, CL Creasy - Nature medicine, 2019 - nature.com
Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

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 …