title: Interfacial peptide inhibitors of HIV-1 integrase activity and dimerization.
abstract: Peptides derived from the interfacial region of dimeric HIV-1 integrase were evaluated as inhibitors of integrase's 3'-endonuclease activity. Three peptides were found to be moderately potent inhibitors with IC(50) values in the low micromolar range. The mode of inhibition was probed through protein crosslinking experiments. Active interfacial peptides were found to inhibit crosslinking of the dimeric form of integrase. Interfacial peptides that were poor inhibitors had no effect on integrase crosslinking.
authors.affiliation: Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
authors.forename: Lei
authors.initials: L
authors.lastname: Zhao
authors.forename: Mary K
authors.initials: MK
authors.lastname: O'Reilly
authors.forename: Michael D
authors.initials: MD
authors.lastname: Shultz
authors.forename: Jean
authors.initials: J
authors.lastname: Chmielewski
mesh_terms: D002851:Chromatography, High Pressure Liquid; D003432:Cross-Linking Reagents; D004591:Electrophoresis, Polyacrylamide Gel; D019427:HIV Integrase / Q000737:chemistry* / Q000187:drug effects / Q000235:genetics; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D008958:Models, Molecular; D009154:Mutation; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D011489:Protein Denaturation
chemical_list: D003432:Cross-Linking Reagents; D019428:HIV Integrase Inhibitors; D010455:Peptides; D019427:HIV Integrase