Elucidating the mechanism by which HIV-1 nucleocapsid mutations confer resistance to integrase strand transfer inhibitors

Persons with HIV (PWH) receiving integrase (IN) strand transfer inhibitors (INSTIs) have been reported to experience virologic failure (VF) in the absence of resistance mutations in IN. We previously reported that mutations in the viral nucleocapsid (NC) are selected in the presence of the INSTI dolutegravir (DTG). Here, we show that these NC mutations accelerate the kinetics of viral DNA integration, suggesting that they limit the window of time available for INSTIs to block viral DNA integration. We find that in primary peripheral blood mononuclear cells, HIV-1 acquires mutations in the viral envelope glycoprotein, NC, and occasionally IN during selection for INSTI resistance. Notably, the selected NC and IN mutations act in concert to reduce the susceptibility of the virus to INSTIs. These results provide insights into the mechanism by which HIV-1 escapes the inhibitory activity of INSTIs and underscore the importance of genotypic analysis outside IN in PWH experiencing VF on INSTI-containing drug regimens.

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Publication Details

Journal
Science Advances
Published
2025-09-12
DOI
https://doi.org/10.1126/sciadv.adz8980
Citations
1
Primary Topic
HIV/AIDS drug development and treatment
Type
article
Field-Weighted Citation Impact
1.40
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article

Elucidating the mechanism by which HIV-1 nucleocapsid mutations confer resistance to integrase strand transfer inhibitors

Xiaolin Wu, Si-Yuan Ding, Yuta Hikichi, Sherimay D. Ablan et al.
1 citations
Science Advances
HIV/AIDS drug development and treatment
1.40
article

Elucidating the mechanism by which HIV-1 nucleocapsid mutations confer resistance to integrase strand transfer inhibitors

Xiaolin Wu, Si-Yuan Ding, Yuta Hikichi, Sherimay D. Ablan, Eric O. Freed, Sean C. Patro, Ryan C. Burdick, Brian T. Luke, Vinay K. Pathak, Erin Clark
article en
1 citations

Abstract

Persons with HIV (PWH) receiving integrase (IN) strand transfer inhibitors (INSTIs) have been reported to experience virologic failure (VF) in the absence of resistance mutations in IN. We previously reported that mutations in the viral nucleocapsid (NC) are selected in the presence of the INSTI dolutegravir (DTG). Here, we show that these NC mutations accelerate the kinetics of viral DNA integration, suggesting that they limit the window of time available for INSTIs to block viral DNA integration. We find that in primary peripheral blood mononuclear cells, HIV-1 acquires mutations in the viral envelope glycoprotein, NC, and occasionally IN during selection for INSTI resistance. Notably, the selected NC and IN mutations act in concert to reduce the susceptibility of the virus to INSTIs. These results provide insights into the mechanism by which HIV-1 escapes the inhibitory activity of INSTIs and underscore the importance of genotypic analysis outside IN in PWH experiencing VF on INSTI-containing drug regimens.

Science AdvancesVol. 11(37)
Frederick National Laboratory for Cancer Research (US), National Cancer Institute (US), Center for Cancer Research (US)
Openalex Percentile: Top 16%
HIV/AIDS drug development and treatment
1.40
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