Ontology highlight
ABSTRACT:
SUBMITTER: Morellato-Castillo L
PROVIDER: S-EPMC3812931 | biostudies-literature | 2013 Jun
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20130611 12
Ligand affinities can be optimized by interfacial cavity filling. A hollow (Phe43 cavity) between HIV-1 surface glycoprotein (gp120) and cluster of differentiation 4 (CD4) receptor extends beyond residue phenylalanine 43 of CD4 and cannot be fully accessed by natural amino acids. To increase HIV-1 gp120 affinity for a family of CD4-mimetic miniproteins (miniCD4s), we targeted the gp120 Phe43 cavity with 11 non-natural phenylalanine derivatives, introduced into a miniCD4 named M48 (1). The best d ...[more]