Antiviral Properties of HIV-1 Capsid Inhibitor GSK878-Reference-Cited by-同舟云学术

Antiviral Properties of HIV-1 Capsid Inhibitor GSK878

Published:2023-05-17 Issue:5 Volume:67 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Wang Chunfu¹^ORCID,Huang Haichang¹,Mallon Kirsten¹,Valera Lourdes¹,Parcella Kyle²,Cockett Mark I.¹,Kadow John F.²,Gillis Eric P.²,Krystal Mark¹^ORCID,Fridell Robert A.¹

Affiliation:

1. Discovery Biology, ViiV Healthcare, Branford, Connecticut, USA

2. Discovery Chemistry, ViiV Healthcare, Branford, Connecticut, USA

Abstract

GSK878 is a newly described HIV-1 inhibitor that binds to the mature capsid (CA) hexamer in a pocket originally identified as the binding site of the well-studied CA inhibitor PF-74. Here, we show that GSK878 is highly potent, inhibiting an HIV-1 reporter virus in MT-2 cells with a mean 50% effective concentration (EC 50 ) of 39 pM and inhibiting a panel of 48 chimeric viruses containing diverse CA sequences with a mean EC 50 of 94 pM.

Funder

ViiV Healthcare

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/aac.01694-22

Reference85 articles.

1. Multiple Roles of HIV-1 Capsid during the Virus Replication Cycle

2. HIV-1 capsid is the key orchestrator of early viral replication

3. HIV-1 Capsid Core: A Bullet to the Heart of the Target Cell

4. HIV Capsid Assembly, Mechanism, and Structure

5. Crystal Structure of Human Cyclophilin A Bound to the Amino-Terminal Domain of HIV-1 Capsid

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