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 …

Drug discovery targeting bromodomain-containing protein 4

Z Liu, P Wang, H Chen, EA Wold, B Tian… - Journal of medicinal …, 2017 - ACS Publications
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …

Current status of latency reversing agents facing the heterogeneity of HIV-1 cellular and tissue reservoirs

A Ait-Ammar, A Kula, G Darcis, R Verdikt… - Frontiers in …, 2020 - frontiersin.org
One of the most explored therapeutic approaches aimed at eradicating HIV-1 reservoirs is
the “shock and kill” strategy which is based on HIV-1 reactivation in latently-infected cells …

HIV “shock and kill” therapy: In need of revision

E Abner, A Jordan - Antiviral research, 2019 - Elsevier
The implementation of antiretroviral therapy 23 years ago has rendered HIV infection
clinically manageable. However, the disease remains incurable, since it establishes latent …

The chemical biology of reversible lysine post-translational modifications

ZA Wang, PA Cole - Cell chemical biology, 2020 - cell.com
Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational
modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein …

Knowledge from London and Berlin: finding threads to a functional HIV cure

J Ding, Y Liu, Y Lai - Frontiers in Immunology, 2021 - frontiersin.org
Despite the ability of combination antiretroviral therapy (cART) to increase the life
expectancy of patients infected with human immunodeficiency virus (HIV), viral reservoirs …

A review of current strategies towards the elimination of latent HIV-1 and subsequent HIV-1 cure

EK Maina, AA Adan, H Mureithi, J Muriuki… - Current HIV …, 2021 - ingentaconnect.com
Background: During the past 35 years, highly effective ART has saved the lives of millions of
people worldwide by suppressing viruses to undetectable levels. However, this does not …

Induction of autophagy by PI3K/MTOR and PI3K/MTOR/BRD4 inhibitors suppresses HIV-1 replication

GR Campbell, RS Bruckman, SD Herns, S Joshi… - Journal of Biological …, 2018 - ASBMB
In this study, we investigated the effects of the dual phosphatidylinositol 3-
kinase/mechanistic target of rapamycin (PI3K/MTOR) inhibitor dactolisib (NVP-BEZ235), the …

BET proteins exhibit transcriptional and functional opposition in the epithelial-to-mesenchymal transition

GP Andrieu, GV Denis - Molecular Cancer Research, 2018 - AACR
Transcriptional programs in embryogenesis and cancer, such as the epithelial-to-
mesenchymal transition (EMT), ensure cellular plasticity, an essential feature of carcinoma …