[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 …

Inhibitors of the HIV-1 capsid, a target of opportunity

SK Carnes, JH Sheehan, C Aiken - Current Opinion in HIV and …, 2018 - journals.lww.com
Small molecules that bind to the viral capsid protein can be potent inhibitors of HIV infection.
Capsid-targeting drugs are predicted to exhibit high barriers to viral resistance, and ongoing …

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 …

A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model

SR Yant, A Mulato, D Hansen, WC Tse… - Nature medicine, 2019 - nature.com
People living with HIV (PLWH) have expressed concern about the life-long burden and
stigma associated with taking pills daily and can experience medication fatigue that might …

Distinct effects of two HIV-1 capsid assembly inhibitor families that bind the same site within the N-terminal domain of the viral CA protein

CT Lemke, S Titolo, U von Schwedler… - Journal of …, 2012 - Am Soc Microbiol
The emergence of resistance to existing classes of antiretroviral drugs necessitates finding
new HIV-1 targets for drug discovery. The viral capsid (CA) protein represents one such …

HIV-1 capsid inhibitors as antiretroviral agents

S Thenin-Houssier, ST Valente - Current HIV research, 2016 - ingentaconnect.com
Background: The infectious human immunodeficiency virus (HIV) particle is characterized by
a conical capsid that encloses the viral RNA genome. The capsid is essential for HIV-1 …

Clinical targeting of HIV capsid protein with a long-acting small molecule

JO Link, MS Rhee, WC Tse, J Zheng, JR Somoza… - Nature, 2020 - nature.com
Oral antiretroviral agents provide life-saving treatments for millions of people living with HIV,
and can prevent new infections via pre-exposure prophylaxis,,,–. However, some people …

[HTML][HTML] 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 …

Antiviral inhibition of the HIV-1 capsid protein

C Tang, E Loeliger, I Kinde, S Kyere, K Mayo… - Journal of molecular …, 2003 - Elsevier
During the assembly stage of the human immunodeficiency virus (HIV) replication cycle,
several thousand copies of the viral Gag polyprotein associate at the cell membrane and …

Small-molecule inhibition of human immunodeficiency virus type 1 infection by virus capsid destabilization

J Shi, J Zhou, VB Shah, C Aiken, K Whitby - Journal of virology, 2011 - Am Soc Microbiol
Human immunodeficiency virus type 1 (HIV-1) infection is dependent on the proper
disassembly of the viral capsid, or “uncoating,” in target cells. The HIV-1 capsid consists of a …