Ebselen, a small-molecule capsid inhibitor of HIV-1 replication

S Thenin-Houssier, IMS De Vera… - Antimicrobial agents …, 2016 - Am Soc Microbiol
The human immunodeficiency virus type 1 (HIV-1) capsid plays crucial roles in HIV-1
replication and thus represents an excellent drug target. We developed a high-throughput …

[HTML][HTML] Rotten to the core: antivirals targeting the HIV-1 capsid core

WM McFadden, AA Snyder, KA Kirby, PR Tedbury… - Retrovirology, 2021 - Springer
The capsid core of HIV-1 is a large macromolecular assembly that surrounds the viral
genome and is an essential component of the infectious virus. In addition to its multiple roles …

An insight on medicinal aspects of novel HIV-1 capsid protein inhibitors

L Sun, X Zhang, S Xu, T Huang, S Song… - European Journal of …, 2021 - Elsevier
A capsid is the protein shell of a virus, encircling its genetic material. The HIV capsid is
erected from a single protein, known as capsid protein. The capsid of HIV-1 significantly …

[HTML][HTML] HIV capsid is a tractable target for small molecule therapeutic intervention

WS Blair, C Pickford, SL Irving, DG Brown… - PLoS …, 2010 - journals.plos.org
Despite a high current standard of care in antiretroviral therapy for HIV, multidrug-resistant
strains continue to emerge, underscoring the need for additional novel mechanism inhibitors …

[HTML][HTML] Exploring modifications of an HIV-1 capsid inhibitor: design, synthesis, and mechanism of action

JP Xu, AC Francis, ME Meuser… - Journal of drug …, 2018 - ncbi.nlm.nih.gov
Recent efforts by both academic and pharmaceutical researchers have focused on the HIV-1
capsid (CA) protein as a new therapeutic target. An interprotomer pocket within the hexamer …

Inhibiting early-stage events in HIV-1 replication by small-molecule targeting of the HIV-1 capsid

S Kortagere, N Madani, MK Mankowski… - Journal of …, 2012 - Am Soc Microbiol
ABSTRACT The HIV-1 capsid (CA) protein plays essential roles in both early and late stages
of virl replication and has emerged as a novel drug target. We report hybrid structure-based …

Inhibition of HIV-1 maturation via small-molecule targeting of the amino-terminal domain in the viral capsid protein

W Wang, J Zhou, UD Halambage, KA Jurado… - Journal of …, 2017 - Am Soc Microbiol
The human immunodeficiency virus type 1 (HIV-1) capsid protein is an attractive therapeutic
target, owing to its multifunctionality in virus replication and the high fitness cost of amino …

Discovery of the human immunodeficiency virus type 1 (HIV-1) attachment inhibitor temsavir and its phosphonooxymethyl prodrug fostemsavir

T Wang, Y Ueda, Z Zhang, Z Yin… - Journal of Medicinal …, 2018 - ACS Publications
The optimization of the 4-methoxy-6-azaindole series of HIV-1 attachment inhibitors (AIs)
that originated with 1 to deliver temsavir (3, BMS-626529) is described. The most beneficial …

Design and synthesis of diselenobisbenzamides (DISeBAs) as nucleocapsid protein 7 (NCp7) inhibitors with anti-HIV activity

L Sancineto, A Mariotti, L Bagnoli, F Marini… - Journal of medicinal …, 2015 - ACS Publications
The interest in the synthesis of Se-containing compounds is growing with the discovery of
derivatives exhibiting various biological activities. In this manuscript, we have identified a …

A small molecule, ACAi-028, with anti-HIV-1 activity targets a novel hydrophobic pocket on HIV-1 capsid

T Chia, T Nakamura, M Amano… - Antimicrobial Agents …, 2021 - Am Soc Microbiol
The human immunodeficiency virus type 1 (HIV-1) capsid (CA) is an essential viral
component of HIV-1 infection and an attractive therapeutic target for antivirals. Here, we …