Ontology highlight
ABSTRACT:
SUBMITTER: Xie H
PROVIDER: S-EPMC2532594 | biostudies-literature | 2007 Oct
REPOSITORIES: biostudies-literature
Xie Hui H Ng Danny D Savinov Sergey N SN Dey Barna B Kwong Peter D PD Wyatt Richard R Smith Amos B AB Hendrickson Wayne A WA
Journal of medicinal chemistry 20070906 20
The first step in HIV infection is the binding of the envelope glycoprotein gp120 to the host cell receptor CD4. An interfacial "Phe43 cavity" in gp120, adjacent to residue Phe43 of gp120-bound CD4, has been suggested as a potential target for therapeutic intervention. We designed a CD4 mutant (D1D2F43C) for site-specific coupling of compounds for screening against the cavity. Altogether, 81 cysteine-reactive compounds were designed, synthesized, and tested. Eight derivatives exceeded the affini ...[more]