A New Family of Small-Molecule CD4-Mimetic Compounds Contacts Highly Conserved Aspartic Acid 368 of HIV-1 gp120 and Mediates Antibody-Dependent Cellular Cytotoxicity

作者：Shilei Ding, Melissa C. Grenier‐Davies, William D. Tolbert, Dani Vézina, Rebekah Sherburn, Jonathan Richard, Jérémie Prévost, Jean-Philippe Chapleau, Gabrielle Gendron‐Lepage, Halima Medjahed, Cameron F. Abrams, Joseph Sodroski, Marzena Pazgier, Amos B. Smith, Andrés Finzi · 发表于：Journal of Virology · 年份：2019 · DOI：10.1128/jvi.01325-19 · 被引用次数：40 · 研究领域：HIV Research and Treatment、Monoclonal and Polyclonal Antibodies Research、HIV/AIDS drug development and treatment

HIV-1 has evolved multiple strategies to avoid humoral responses. One efficient mechanism is to keep its envelope glycoprotein (Env) in its "closed" conformation. Here, we report on a new family of small molecules that are able to "open up" Env, thus exposing vulnerable epitopes. This new family of molecules binds in the Phe43 cavity and contacts the highly conserved D368 residue. The structural and biological attributes of molecules of this family make them good candidates for drug development.