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 …

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 …

International AIDS Society global scientific strategy: towards an HIV cure 2016

SG Deeks, SR Lewin, AL Ross, J Ananworanich… - Nature medicine, 2016 - nature.com
Antiretroviral therapy is not curative. Given the challenges in providing lifelong therapy to a
global population of more than 35 million people living with HIV, there is intense interest in …

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 …

Single-cell RNA-seq highlights intratumoral heterogeneity in primary glioblastoma

AP Patel, I Tirosh, JJ Trombetta, AK Shalek… - Science, 2014 - science.org
Human cancers are complex ecosystems composed of cells with distinct phenotypes,
genotypes, and epigenetic states, but current models do not adequately reflect tumor …

The mechanisms behind the therapeutic activity of BET bromodomain inhibition

J Shi, CR Vakoc - Molecular cell, 2014 - cell.com
The bromodomain and extraterminal (BET) protein Brd4 recruits transcriptional regulatory
complexes to acetylated chromatin. While Brd4 is considered to be a general transcriptional …

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 …

Activation of HIV transcription with short-course vorinostat in HIV-infected patients on suppressive antiretroviral therapy

JH Elliott, F Wightman, A Solomon, K Ghneim… - PLoS …, 2014 - journals.plos.org
Human immunodeficiency virus (HIV) persistence in latently infected resting memory CD4+
T-cells is the major barrier to HIV cure. Cellular histone deacetylases (HDACs) are important …

Ex vivo analysis identifies effective HIV-1 latency–reversing drug combinations

GM Laird, CK Bullen, DIS Rosenbloom… - The Journal of …, 2015 - Am Soc Clin Investig
Reversal of HIV-1 latency by small molecules is a potential cure strategy. This approach will
likely require effective drug combinations to achieve high levels of latency reversal. Using …