[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 …
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 …
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 …
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 …
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 …
that bind acetylated histones through their bromodomains to regulate gene transcription …
[HTML][HTML] A phase separation model for transcriptional control
Phase-separated multi-molecular assemblies provide a general regulatory mechanism to
compartmentalize biochemical reactions within cells. We propose that a phase separation …
compartmentalize biochemical reactions within cells. We propose that a phase separation …
[HTML][HTML] Transcriptional addiction in cancer
Cancer arises from genetic alterations that invariably lead to dysregulated transcriptional
programs. These dysregulated programs can cause cancer cells to become highly …
programs. These dysregulated programs can cause cancer cells to become highly …
Plasticity in binding confers selectivity in ligand-induced protein degradation
Heterobifunctional small-molecule degraders that induce protein degradation through ligase-
mediated ubiquitination have shown considerable promise as a new pharmacological …
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 …
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 …
gene expression and are involved in cancer pathogenesis. Over the last years, several BET …