title: Sidechain-linked inhibitors of HIV-1 protease dimerization.
abstract: There is a great need for alternative modes of inhibition for the design of anti-HIV therapies, due to the increased resistance of HIV to currently approved drugs. A novel strategy for generating potent dimerization inhibitors of HIV-1 protease is described based on sidechain-linked interfacial peptides. In a number of cases the activity of these agents against HIV-1 protease was found to be among the most potent reported, with inhibitory constants in the low nM range.
authors.affiliation: Department of Chemistry, 560 Oval Drive, Purdue University, West Lafayette, IN 47907, USA.
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Bowman
authors.forename: Jean
authors.initials: J
authors.lastname: Chmielewski
mesh_terms: D003432:Cross-Linking Reagents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D019281:Dimerization; D016333:HIV Protease / Q000737:chemistry / Q000378:metabolism*; D017320:HIV Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D007700:Kinetics
chemical_list: D003432:Cross-Linking Reagents; D017320:HIV Protease Inhibitors; D016333:HIV Protease; C514803:p16 protease, Human immunodeficiency virus 1