PMID: 9539708May 16, 1998Paper

Identification of a nucleotide binding site in HIV-1 integrase

Proceedings of the National Academy of Sciences of the United States of America
R R DrakeY Pommier

Abstract

HIV-1 integrase is essential for viral replication and can be inhibited by antiviral nucleotides. Photoaffinity labeling with the 3'-azido-3'-deoxythymidine (AZT) analog 3',5-diazido-2', 3'-dideoxyuridine 5'-monophosphate (5N3-AZTMP) and proteolytic mapping identified the amino acid 153-167 region of integrase as the site of photocrosslinking. Docking of 5N3-AZTMP revealed the possibility for strong hydrogen bonds between the inhibitor and lysines 156, 159, and 160 of the enzyme. Mutation of these residues reduced photocrosslinking selectively. This report elucidates the binding site of a nucleotide inhibitor of HIV-1 integrase, and possibly a component of the enzyme polynucleotide binding site.

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Citations

Dec 3, 2008·Journal of Molecular Modeling·Devendra K DhakedEvans C Coutinho
Sep 7, 2000·Antiviral Research·Y PommierN Neamati
May 23, 2001·Pathologie-biologie·J d'AngeloH Leh
Jan 5, 1999·Bioorganic & Medicinal Chemistry Letters·J ZhangV Nair
Mar 4, 2000·Bioorganic & Medicinal Chemistry Letters·M TaktakishviliV Nair
Aug 5, 1999·Nucleosides & Nucleotides·G Abu SheikaP La Colla
Oct 8, 2009·Nucleic Acids Research·Zeina HobaikaSerge Fermandjian
Dec 19, 2008·Retrovirology·Olivier DelelisJean-François Mouscadet
Jun 21, 2006·Proceedings of the National Academy of Sciences of the United States of America·Laith Q Al-MawsawiNouri Neamati
Feb 15, 2001·Expert Opinion on Investigational Drugs·N Neamati
Nov 19, 2008·Journal of Molecular Biology·James DolanJonathan Leis
Jan 24, 2003·Expert Opinion on Therapeutic Targets·Khampoune SayasithJocelyn Yelle
Sep 12, 2002·Expert Opinion on Therapeutic Targets·M L AndréolaS Litvak
Dec 19, 2007·Advances in Pharmacology·Elena A SemenovaYves Pommier
Aug 17, 2005·Journal of Biomolecular Screening·Sinu JohnColleen B Jonsson
May 10, 2000·The Journal of Biological Chemistry·N JingY Pommier
Jan 15, 2004·Molecular Pharmacology·Eric DeprezJean-François Mouscadet
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Jun 10, 2004·Antiviral Chemistry & Chemotherapy·Mario SechiNouri Neamati
Mar 12, 2020·Journal of Chemical Information and Modeling·Sugunadevi SakkiahHuixiao Hong
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Nov 7, 2000·Journal of Medicinal Chemistry·C A SotrifferJ A McCammon
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