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Journal article
Optimization of Small Molecules That Sensitize HIV‑1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity
ACS medicinal chemistry letters, v 11(3), pp 371-378
12 Mar 2020
PMID: 32184972
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
With approximately 37 million people living with HIV worldwide and an estimated 2 million new infections reported each year, the need to derive novel strategies aimed at eradicating HIV-1 infection remains a critical worldwide challenge. One potential strategy would involve eliminating infected cells via antibody-dependent cellular cytotoxicity (ADCC). HIV-1 has evolved sophisticated mechanisms to conceal epitopes located in its envelope glycoprotein (Env) that are recognized by ADCC-mediating antibodies present in sera from HIV-1 infected individuals. Our aim is to circumvent this evasion via the development of small molecules that expose relevant anti-Env epitopes and sensitize HIV-1 infected cells to ADCC. Rapid elaboration of an initial screening hit using parallel synthesis and structure-based optimization has led to the development of potent small molecules that elicit this humoral response. Efforts to increase the ADCC activity of this class of small molecules with the aim of increasing their therapeutic potential was based on our recent cocrystal structures with gp120 core.
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Details
- Title
- Optimization of Small Molecules That Sensitize HIV‑1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity
- Creators
- Melissa C Grenier - University of PennsylvaniaShilei Ding - University of MontrealDani Vézina - University of MontrealJean-Philippe Chapleau - University of MontrealWilliam D Tolbert - Uniformed Services University of the Health SciencesRebekah Sherburn - Uniformed Services University of the Health SciencesArne Schön - Johns Hopkins UniversitySambasivarao Somisetti - Drexel UniversityCameron F Abrams - Drexel UniversityMarzena Pazgier - Uniformed Services University of the Health SciencesAndrés Finzi - University of MontrealAmos B Smith - University of Pennsylvania
- Publication Details
- ACS medicinal chemistry letters, v 11(3), pp 371-378
- Publisher
- American Chemical Society; Washington, DC
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Chemical and Biological Engineering
- Web of Science ID
- WOS:000526401400030
- Scopus ID
- 2-s2.0-85075625748
- Other Identifier
- 991019168593304721
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- Collaboration types
- Domestic collaboration
- International collaboration
- Web of Science research areas
- Chemistry, Medicinal