Long Dissociation of Bictegravir from HIV-1 Integrase-DNA Complexes | Zendy

Kirsten L. White | Zendy; Nathan Osman | Zendy; Ernesto Cuadra-Foy | Zendy; Bluma Brenner | Zendy; Devleena Shivakumar | Zendy; Federico Campigotto | Zendy; Manuel Tsiang | Zendy; Philip Morganelli | Zendy; Nikolai Novikov | Zendy; Scott E. Lazerwith | Zendy; Haolun Jin | Zendy; Anita NiedzielaMajka | Zendy

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Long Dissociation of Bictegravir from HIV-1 Integrase-DNA Complexes

Author(s) -

Kirsten L. White,

Nathan Osman,

Ernesto Cuadra-Foy,

Bluma Brenner,

Devleena Shivakumar,

Federico Campigotto,

Manuel Tsiang,

Philip Morganelli,

Nikolai Novikov,

Scott E. Lazerwith,

Haolun Jin,

Anita NiedzielaMajka

Publication year - 2021

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.02406-20

Subject(s) - elvitegravir , dolutegravir , integrase , raltegravir , mutant , chemistry , virology , integrase inhibitor , dna , stereochemistry , pharmacology , biology , human immunodeficiency virus (hiv) , viral load , biochemistry , antiretroviral therapy , gene

The HIV integrase (IN) strand transfer inhibitor (INSTI) bictegravir (BIC) has a long dissociation half-life ( t 1/2 ) from wild-type IN-DNA complexes: BIC 163 h > dolutegravir (DTG) 96 h > raltegravir (RAL) 10 h > elvitegravir (EVG) 3.3 h. In cells, BIC had more durable antiviral activity against wild-type HIV after drug washout than RAL or EVG.

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