PMID: 9420029Jan 7, 1998Paper

Sensitivity of human immunodeficiency virus to bicyclam derivatives is influenced by the three-dimensional structure of gp120

Antimicrobial Agents and Chemotherapy
K De VreeseE De Clercq

Abstract

The bicyclams are a new class of anti-human immunodeficiency virus (anti-HIV) compounds targeted at viral entry. From marker rescue experiments, it appears that the envelope gp120 glycoprotein plays an important role in the anti-HIV activity of the bicyclams. Bicyclam-resistant strains contain a number of amino acid changes scattered over the V2 to V5 region of gp120. Experiments aimed at estimating the relative importance of particular amino acid changes with regard to the overall resistance pattern are described. The sequences of some partially bicyclam-resistant virus strains, obtained during the resistance development process, were analyzed, and the corresponding 50% effective concentrations were determined. Selected mutations observed in bicyclam-resistant strains were introduced in the wild-type background by site-directed mutagenesis. In addition, some amino acids were back-mutated to their wild-type counterparts in an otherwise JM3100-resistant strain. The sensitivities of these mutant viruses to bicyclams were determined. Construction of chimeric viruses, carrying the V3 loop of JM3100-resistant virus in a wild-type HIV type 1 HXB2 background, enabled us to investigate the importance of the mutations in the V3 loop of ...Continue Reading

References

Jun 15, 1992·Proceedings of the National Academy of Sciences of the United States of America·E De ClercqD Schwartz
Aug 1, 1988·Journal of Virological Methods·R PauwelsE De Clercq
Feb 3, 1995·The Journal of Biological Chemistry·P CatastiG Gupta
Apr 1, 1994·Antimicrobial Agents and Chemotherapy·E De ClercqR Datema
May 10, 1994·Proceedings of the National Academy of Sciences of the United States of America·H J RyserG J DiSciullo

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Citations

Jun 20, 2003·Nature Reviews. Drug Discovery·Erik De Clercq
Jul 5, 2005·Expert Opinion on Investigational Drugs·J M Kilby
Jul 21, 2010·Antimicrobial Agents and Chemotherapy·Emmanuel González-OrtegaJosé A Esté
Jan 24, 2003·Expert Opinion on Therapeutic Targets·Lokesh AgrawalLokesh Agrawal
Jun 17, 2020·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Jingzhe WangHuabiao Chen
Sep 19, 2006·Seminars in Immunology·Fernando Arenzana-Seisdedos, Marc Parmentier

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