HIV-1 Integrase Inhibitors That Are Active against Drug-Resistant Integrase Mutants.

Drug Resistance, Viral / genetics HIV Infections / drug therapy HIV Integrase / genetics HIV Integrase Inhibitors / pharmacology HIV-1 / genetics Heterocyclic Compounds, 3-Ring / pharmacology Humans Oxazines / pharmacology Pharmaceutical Preparations Piperazines / pharmacology Pyridones / pharmacology
drug resistance human immunodeficiency virus inhibitor integrase replication capacity

Journal

Antimicrobial agents and chemotherapy
ISSN: 1098-6596
Titre abrégé: Antimicrob Agents Chemother
Pays: United States
ID NLM: 0315061

Informations de publication

Date de publication:
20 08 2020
Historique:
received: 01 04 2020
accepted: 25 06 2020
pubmed: 1 7 2020
medline: 22 6 2021
entrez: 1 7 2020
Statut: epublish

Résumé

The currently recommended first-line therapy for HIV-1-infected patients is an integrase (IN) strand transfer inhibitor (INSTI), either dolutegravir (DTG) or bictegravir (BIC), in combination with two nucleoside reverse transcriptase inhibitors (NRTIs). Both DTG and BIC potently inhibit most INSTI-resistant IN mutants selected by the INSTIs raltegravir (RAL) and elvitegravir (EVG). BIC has not been reported to select for resistance in treatment-naive patients, and DTG has selected for a small number of resistant viruses in treatment-naive patients. However, some patients who had viruses with substitutions selected by RAL and EVG responded poorly when switched to DTG-based therapies, and there are mutants that cause a considerable decrease in the potencies of DTG and BIC in

Identifiants

DOI: 10.1128/AAC.00611-20 PMID: 32601157 PMC: PMC7449158
pubmed: 32601157
pii: AAC.00611-20
doi: 10.1128/AAC.00611-20
pmc: PMC7449158
pii:
doi:

Substances chimiques

HIV Integrase Inhibitors 0
Heterocyclic Compounds, 3-Ring 0
Oxazines 0
Pharmaceutical Preparations 0
Piperazines 0
Pyridones 0
HIV Integrase EC 2.7.7.-

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, N.I.H., Intramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : NIAID NIH HHS
ID : R01 AI136680
Pays : United States
Organisme : NIGMS NIH HHS
ID : P30 GM103331
Pays : United States
Organisme : NIGMS NIH HHS
ID : U54 GM103368
Pays : United States
Organisme : NCI NIH HHS
ID : P30 CA014195
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI146017
Pays : United States
Organisme : NIAID NIH HHS
ID : U54 AI150472
Pays : United States

Informations de copyright

Copyright © 2020 American Society for Microbiology.

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Auteurs

Steven J Smith (SJ)

HIV Dynamics and Replication Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland, USA.

Xue Zhi Zhao (XZ)

Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, Maryland, USA.

Dario Oliveira Passos (DO)

Laboratory of Genetics, The Salk Institute for Biological Studies, La Jolla, California, USA.

Dmitry Lyumkis (D)

Laboratory of Genetics, The Salk Institute for Biological Studies, La Jolla, California, USA.
Department of Structural and Computational Biology, The Scripps Research Institute, La Jolla, California, USA.

Terrence R Burke (TR)

Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, Maryland, USA.

Stephen H Hughes (SH)

HIV Dynamics and Replication Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland, USA hughesst@mail.nih.gov.
ORCID: 0000-0002-9176-4377

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Classifications MeSH

questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Résistance aux substances › Résistance microbienne aux médicaments › Résistance virale aux médicaments › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Maladies du système immunitaire › Déficits immunitaires › Infections à VIH › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines virales › Protéines virales structurales › Protéines nucléocapside › Protéines du core viral › Produits du gène pol › Produits du gène pol du virus de l'immunodéficience humaine › Intégrase du VIH › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiviraux › Antirétroviraux › Agents antiVIH › Inhibiteurs de l'intégrase du VIH › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Virus › Virus à ARN › Retroviridae › Lentivirus › Lentivirus des primates › VIH (Virus de l'Immunodéficience Humaine) › VIH-1 (Virus de l'Immunodéficience Humaine de type 1) › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérocycliques 3 noyaux › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Oxazines › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Préparations pharmaceutiques › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pipérazines › HIV-1 Integrase Inhibitors That Are Active...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyridines › Pyridones › HIV-1 Integrase Inhibitors That Are Active...