Structure-activity relationships in the binding of chemically derivatized CD4 to gp120 from human immunodeficiency virus

…, D Ng, SN Savinov, B Dey, PD Kwong…

Index: Xie, Hui; Ng, Danny; Savinov, Sergey N.; Dey, Barna; Kwong, Peter D.; Wyatt, Richard; Smith III, Amos B.; Hendrickson, Wayne A. Journal of Medicinal Chemistry, 2007 , vol. 50, # 20 p. 4898 - 4908

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Citation Number: 44

Abstract

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, ...