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 …
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 …
Drug discovery targeting bromodomain-containing protein 4
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 …
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
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 …
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
The implementation of antiretroviral therapy 23 years ago has rendered HIV infection
clinically manageable. However, the disease remains incurable, since it establishes latent …
clinically manageable. However, the disease remains incurable, since it establishes latent …
The chemical biology of reversible lysine post-translational modifications
Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational
modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein …
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 …
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 …
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 …
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 …
mesenchymal transition (EMT), ensure cellular plasticity, an essential feature of carcinoma …