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Recognition of HIV-inactivating peptide triazoles by the recombinant soluble Env trimer, BG505 SOSIP.664
Journal article   Open access   Peer reviewed

Recognition of HIV-inactivating peptide triazoles by the recombinant soluble Env trimer, BG505 SOSIP.664

Kriti Acharya, Adel A Rashad, Francesca Moraca, Per Johan Klasse, John P Moore, Cameron Abrams and Irwin Chaiken
Proteins, structure, function, and bioinformatics, v 85(5), pp 843-851
May 2017
PMID: 28056499
url
https://doi.org/10.1002/prot.25238View
Published, Version of Record (VoR) Open

Abstract

HIV Envelope Protein gp120 - genetics Cricetulus Triazoles - chemistry Humans Protein Multimerization HIV Envelope Protein gp120 - antagonists & inhibitors HIV Envelope Protein gp120 - metabolism Peptides - chemical synthesis Antiviral Agents - chemistry HIV-1 - chemistry Triazoles - chemical synthesis Protein Interaction Domains and Motifs HIV Envelope Protein gp120 - chemistry Binding Sites CHO Cells Binding, Competitive Protein Structure, Tertiary Recombinant Proteins - metabolism Protein Conformation, alpha-Helical Gene Expression Enzyme-Linked Immunosorbent Assay Peptides - chemistry Solubility Recombinant Proteins - chemistry Recombinant Proteins - genetics Molecular Dynamics Simulation Animals Protein Conformation, beta-Strand Antibodies, Viral - chemistry Antiviral Agents - chemical synthesis Protein Binding Molecular Docking Simulation Kinetics
Peptide triazole (PT) antagonists interact with gp120 subunits of HIV-1 Env trimers to block host cell receptor interactions, trigger gp120 shedding, irreversibly inactivate virus and inhibit infection. Despite these enticing functions, understanding the structural mechanism of PT-Env trimer encounter has been limited. In this work, we combined competition interaction analysis and computational simulation to demonstrate PT binding to the recombinant soluble trimer, BG505 SOSIP.664, a stable variant that resembles native virus spikes in binding to CD4 receptor as well as known conformationally-dependent Env antibodies. Binding specificity and computational modeling fit with encounter through complementary PT pharmacophore Ile-triazolePro-Trp interaction with a 2-subsite cavity in the Env gp120 subunit of SOSIP trimer similar to that in monomeric gp120. These findings argue that PTs are able to recognize and bind a closed prefusion state of Env trimer upon HIV-1 encounter. The results provide a structural model of how PTs exert their function on virion trimeric spike protein and a platform to inform future antagonist design. Proteins 2017; 85:843-851. © 2016 Wiley Periodicals, Inc.

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Collaboration types
Domestic collaboration
Web of Science research areas
Biochemistry & Molecular Biology
Biophysics
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