ArticleJournal of virology2013
Antibody conjugation approach enhances breadth and potency of neutralization of anti-HIV-1 antibodies and CD4-IgG.
Article in Journal of virology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 22 citations in OpenAlex.
- Multimerization and Conjugation to Antiviral and Cytotoxic Payloads Enhance the Activity of Virus-Neutralizing Nanobodies In Vitro.ACS omega · 2026Article
- Bioorthogonal Reaction of o-Quinone with Furan-2(3H)-One for Site-Selective Tyrosine Conjugation and Construction of Bispecific Antibody Complexes.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Nonperturbative Fluorogenic Labeling of Immunophilins Enables the Wash-free Detection of Immunosuppressants.ACS central science · 2024Article
- Site-Selective Tyrosine Reaction for Antibody-Cell Conjugation and Targeted Immunotherapy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Recent developments in chemical conjugation strategies targeting native amino acids in proteins and their applications in antibody-drug conjugates.Chemical science · 2021Review
- Engineering broadly neutralizing antibodies for HIV prevention and therapy.Advanced drug delivery reviews · 2016Review
- Antibody engineering for increased potency, breadth and half-life.Current opinion in HIV and AIDS · 2015Review
- Chemical and Structural Aspects of Ebola Virus Entry Inhibitors.ACS infectious diseases · 2015Article
- Click chemistry in complex mixtures: bioorthogonal bioconjugation.Chemistry & biology · 2014Review
- Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc.ACS medicinal chemistry letters · 2014Article
- Rapid, stable, chemoselective labeling of thiols with Julia-Kocieński-like reagents: a serum-stable alternative to maleimide-based protein conjugation.Angewandte Chemie (International ed. in English) · 2013Article
- Chemically Programmed Antibodies AS HIV-1 Attachment Inhibitors.ACS medicinal chemistry letters · 2013Article
Corrections and comments
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Authors and funding
11 authors at 6 institutions in 2 countries.
Funding
Abstract
Broadly neutralizing antibodies PG9 and PG16 effectively neutralize 70 to 80% of circulating HIV-1 isolates. In this study, the neutralization abilities of PG9 and PG16 were further enhanced by bioconjugation with aplaviroc, a small-molecule inhibitor of virus entry into host cells. A novel air-stable diazonium hexafluorophosphate reagent that allows for rapid, tyrosine-selective functionalization of proteins and antibodies under mild conditions was used to prepare a series of aplaviroc-conjugated antibodies, including b12, 2G12, PG9, PG16, and CD4-IgG. The conjugated antibodies blocked HIV-1 entry through two mechanisms: by binding to the virus itself and by blocking the CCR5 receptor on host cells. Chemical modification did not significantly alter the potency of the parent antibodies against nonresistant HIV-1 strains. Conjugation did not alter the pharmacokinetics of a model IgG in blood. The PG9-aplaviroc conjugate was tested against a panel of 117 HIV-1 strains and was found to neutralize 100% of the viruses. PG9-aplaviroc conjugate IC50s were lower than those of PG9 in neutralization studies of 36 of the 117 HIV-1 strains. These results support this new approach to bispecific antibodies and offer a potential new strategy for combining HIV-1 therapies.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.