The structural and mechanistic bases for the viral resistance to allosteric HIV-1 integrase inhibitor pirmitegravir.
Autor: | Dinh T; Division of Infectious Diseases, University of Colorado Anschutz Medical Campus, Aurora, Colorado, USA., Tber Z; Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, Atlanta, Georgia, USA., Rey JS; Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware, USA., Mengshetti S; Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, Atlanta, Georgia, USA., Annamalai AS; Division of Infectious Diseases, University of Colorado Anschutz Medical Campus, Aurora, Colorado, USA., Haney R; Division of Infectious Diseases, University of Colorado Anschutz Medical Campus, Aurora, Colorado, USA., Briganti L; Division of Infectious Diseases, University of Colorado Anschutz Medical Campus, Aurora, Colorado, USA., Amblard F; Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, Atlanta, Georgia, USA., Fuchs JR; College of Pharmacy, The Ohio State University, Columbus, Ohio, United States., Cherepanov P; Chromatin Structure & Mobile DNA Laboratory, The Francis Crick Institute, London, United Kingdom., Kim K; ST Pharm Co., Ltd., Seoul, South Korea., Schinazi RF; Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, Atlanta, Georgia, USA., Perilla JR; Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware, USA., Kim B; Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, Atlanta, Georgia, USA., Kvaratskhelia M; Division of Infectious Diseases, University of Colorado Anschutz Medical Campus, Aurora, Colorado, USA. |
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Jazyk: | angličtina |
Zdroj: | BioRxiv : the preprint server for biology [bioRxiv] 2024 Jan 26. Date of Electronic Publication: 2024 Jan 26. |
DOI: | 10.1101/2024.01.26.577387 |
Abstrakt: | Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are investigational antiretroviral agents which potently impair virion maturation by inducing hyper-multimerization of IN and inhibiting its interaction with viral genomic RNA. The pyrrolopyridine-based ALLINI pirmitegravir (PIR) has recently advanced into Phase 2a clinical trials. Previous cell culture based viral breakthrough assays identified the HIV-1 Competing Interests: Conflict of interest statement The authors declare a conflict of interest. Kyungjin Kim is the Chief Executive Officer of ST Pharm Co. Ltd. No other authors declare a potential conflict of interest. |
Databáze: | MEDLINE |
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