Block-and-lock strategies to cure HIV infection
G Vansant, A Bruggemans, J Janssens, Z Debyser - Viruses, 2020 - mdpi.com
Today HIV infection cannot be cured due to the presence of a reservoir of latently infected
cells inducing a viral rebound upon treatment interruption. Hence, the latent reservoir is …
cells inducing a viral rebound upon treatment interruption. Hence, the latent reservoir is …
The current status of latency reversing agents for HIV-1 remission
A Rodari, G Darcis, CM Van Lint - Annual review of virology, 2021 - annualreviews.org
Combinatory antiretroviral therapy (cART) reduces human immunodeficiency virus type 1
(HIV-1) replication but is not curative because cART interruption almost invariably leads to a …
(HIV-1) replication but is not curative because cART interruption almost invariably leads to a …
Targeting bromodomain and extraterminal proteins for drug discovery: from current progress to technological development
P Tang, J Zhang, J Liu, CM Chiang… - Journal of medicinal …, 2021 - ACS Publications
Bromodomain and extraterminal (BET) proteins bind acetylated lysine residues in histones
and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics …
and nonhistone proteins via tandem bromodomains and regulate chromatin dynamics …
Block-and-lock: new horizons for a cure for HIV-1
I Moranguinho, ST Valente - Viruses, 2020 - mdpi.com
HIV-1/AIDS remains a global public health problem. The world health organization (WHO)
reported at the end of 2019 that 38 million people were living with HIV-1 worldwide, of which …
reported at the end of 2019 that 38 million people were living with HIV-1 worldwide, of which …
Block and lock HIV cure strategies to control the latent reservoir
CL Ahlenstiel, G Symonds, SJ Kent… - Frontiers in cellular and …, 2020 - frontiersin.org
The HIV latent reservoir represents the major challenge to cure development. Residing in
resting CD4+ T cells and myeloid cells at multiple locations in the body, including sanctuary …
resting CD4+ T cells and myeloid cells at multiple locations in the body, including sanctuary …
Bromodomain inhibitors and therapeutic applications
BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …
and plays a fundamental role in chromatin-based cellular processes including gene …
Drug discovery targeting nuclear receptor binding SET domain protein 2 (NSD2)
Nuclear receptor binding SET domain proteins (NSDs) catalyze the mono-or dimethylation
of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S-adenosyl-l-methionine (SAM) …
of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S-adenosyl-l-methionine (SAM) …
An updated patent review of BRD4 degraders
Introduction Bromodomain-containing protein 4 (BRD4), an important epigenetic reader, is
closely associated with the pathogenesis and development of many diseases, including …
closely associated with the pathogenesis and development of many diseases, including …
Discovery, X-ray crystallography, and anti-inflammatory activity of bromodomain-containing protein 4 (BRD4) BD1 inhibitors targeting a distinct new binding site
Bromodomain-containing protein 4 (BRD4) is an emerging epigenetic drug target for
intractable inflammatory disorders. The lack of highly selective inhibitors among BRD4 …
intractable inflammatory disorders. The lack of highly selective inhibitors among BRD4 …
Discovery of orally bioavailable chromone derivatives as potent and selective BRD4 inhibitors: scaffold hop**, optimization, and pharmacological evaluation
Bromodomain-containing protein 4 (BRD4) represents a promising drug target for anti-
inflammatory therapeutics. Herein, we report the design, synthesis, and pharmacological …
inflammatory therapeutics. Herein, we report the design, synthesis, and pharmacological …