GS-CA compounds: first-in-class HIV-1 capsid inhibitors covering multiple grounds

K Singh, F Gallazzi, KJ Hill, DH Burke… - Frontiers in …, 2019 - frontiersin.org
Recently reported HIV-1 capsid (CA) inhibitors GS-CA1 and GS-6207 (an analog of GS-
CA1) are first-in-class compounds with long-acting potential. Reportedly, both compounds …

HIV capsid inhibitors beyond PF74

C McArthur, F Gallazzi, TP Quinn, K Singh - Diseases, 2019 - mdpi.com
Human immunodeficiency virus (HIV) capsid plays important roles at multiple stages of viral
replication. At the initial stages, controlled uncoating (disassembly) of the capsid ensures …

[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 …

Discovery of novel 1, 2, 4‐triazole phenylalanine derivatives targeting an unexplored region within the interprotomer pocket of the HIV capsid protein

X Jiang, PP Sharma, B Rathi, X Ji, L Hu… - Journal of medical …, 2022 - Wiley Online Library
Human immunodeficiency virus (HIV) capsid (CA) protein is a promising target for
developing novel anti‐HIV drugs. Starting from highly anticipated CA inhibitors PF‐74, we …

Novel inhibitor binding site discovery on HIV-1 capsid N-terminal domain by NMR and X-ray crystallography

N Goudreau, CT Lemke, AM Faucher… - ACS chemical …, 2013 - ACS Publications
The HIV-1 capsid (CA) protein, a domain of Gag, which participates in formation of both the
mature and immature capsid, represents a potential target for anti-viral drug development …

Toward structurally novel and metabolically stable HIV-1 capsid-targeting small molecules

SKV Vernekar, RL Sahani, MC Casey, J Kankanala… - Viruses, 2020 - mdpi.com
HIV-1 capsid protein (CA) plays an important role in many steps of viral replication and
represents an appealing antiviral target. Several CA-targeting small molecules of various …

Capsid (CA) protein as a novel drug target: recent progress in the research of HIV-1 CA inhibitors.

J Zhang, X Liu, E De Clercq - Mini reviews in medicinal chemistry, 2009 - europepmc.org
The capsid (CA) protein is the major structural component of HIV-1 and plays a key role in
the regulation of viral life cycle. Inhibition of CA will affect the viral assembly and budding …

Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors

X Zhang, L Sun, ME Meuser, WA Zalloum, S Xu… - European journal of …, 2021 - Elsevier
Abstract HIV-1 capsid (CA) plays indispensable and multiple roles in the life cycle of HIV-1,
become an attractive target in antiviral therapy. Herein, we report the design, synthesis, and …

Design, synthesis and structure-activity relationships of 4-phenyl-1H-1, 2, 3-triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral …

L Sun, T Huang, A Dick, ME Meuser… - European journal of …, 2020 - Elsevier
HIV-1 CA is involved in different stages of the viral replication cycle, performing essential
roles in both early (uncoating, reverse transcription, nuclear import, integration) and late …

Design, synthesis, and mechanism study of benzenesulfonamide-containing phenylalanine derivatives as novel HIV-1 capsid inhibitors with improved antiviral …

L Sun, A Dick, ME Meuser, T Huang… - Journal of medicinal …, 2020 - ACS Publications
The HIV-1 CA protein has gained remarkable attention as a promising therapeutic target for
the development of new antivirals, due to its pivotal roles in HIV-1 replication (structural and …