ArticleJournal of virology2007
X-ray crystal structures of human immunodeficiency virus type 1 protease mutants complexed with atazanavir.
Article in Journal of virology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 35 citations in OpenAlex.
- Article
- Article
- Computer-Aided Prediction of the Interactions of Viral Proteases with Antiviral Drugs: Antiviral Potential of Broad-Spectrum Drugs.Molecules (Basel, Switzerland) · 2023Article
- GSK3640254 Is a Novel HIV-1 Maturation Inhibitor with an Optimized Virology Profile.Antimicrobial agents and chemotherapy · 2022Article
- Structural analyses of 2015-updated drug-resistant mutations in HIV-1 protease: an implication of protease inhibitor cross-resistance.BMC bioinformatics · 2016Article
- Mechanistic Studies and Modeling Reveal the Origin of Differential Inhibition of Gag Polymorphic Viruses by HIV-1 Maturation Inhibitors.PLoS pathogens · 2016Article
- Identification and Characterization of BMS-955176, a Second-Generation HIV-1 Maturation Inhibitor with Improved Potency, Antiviral Spectrum, and Gag Polymorphic Coverage.Antimicrobial agents and chemotherapy · 2016Article
- Heteroaromatic π-stacking energy landscapes.Journal of chemical information and modeling · 2014Article
- Automating crystallographic structure solution and refinement of protein-ligand complexes.Acta crystallographica. Section D, Biological crystallography · 2014Article
- Ligand placement based on prior structures: the guided ligand-replacement method.Acta crystallographica. Section D, Biological crystallography · 2014Article
- Elucidating a relationship between conformational sampling and drug resistance in HIV-1 protease.Biochemistry · 2013Article
- A switch-on mechanism to activate maize ribosome-inactivating protein for targeting HIV-infected cells.Nucleic acids research · 2010Article
- Rationale for more diverse inhibitors in competition with substrates in HIV-1 protease.Biophysical journal · 2010Article
- Atazanavir: its role in HIV treatment.Expert review of anti-infective therapy · 2008Review
- Effect of the active site D25N mutation on the structure, stability, and ligand binding of the mature HIV-1 protease.The Journal of biological chemistry · 2008Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Atazanavir, which is marketed as REYATAZ, is the first human immunodeficiency virus type 1 (HIV-1) protease inhibitor approved for once-daily administration. As previously reported, atazanavir offers improved inhibitory profiles against several common variants of HIV-1 protease over those of the other peptidomimetic inhibitors currently on the market. This work describes the X-ray crystal structures of complexes of atazanavir with two HIV-1 protease variants, namely, (i) an enzyme optimized for resistance to autolysis and oxidation, referred to as the cleavage-resistant mutant (CRM); and (ii) the M46I/V82F/I84V/L90M mutant of the CRM enzyme, which is resistant to all approved HIV-1 protease inhibitors, referred to as the inhibitor-resistant mutant. In these two complexes, atazanavir adopts distinct bound conformations in response to the V82F substitution, which may explain why this substitution, at least in isolation, has yet to be selected in vitro or in the clinic. Because of its nearly symmetrical chemical structure, atazanavir is able to make several analogous contacts with each monomer of the biological dimer.
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