title: Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.
abstract: Dimers of known HIV-1 integrase inhibitory hexapeptide H-His-Cys-Lys-Phe-Trp-Trp-NH(2) containing different lengths of cross linkers in the place of cysteine residue, were designed, and synthesized. The inhibitory potency of these dimeric peptides is consistently higher than the lead hexapeptide. The dimeric peptide with djenkolic acid linker exhibited IC(50) values of 5.3 and 6.5 microM, for 3'-end processing and strand transfer, respectively.
authors.affiliation: Laboratory of Medicinal Chemistry, CCR, NCI-Frederick, NIH, Frederick, MD 21702, USA.
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Krajewski
authors.forename: Ya-Qiu
authors.initials: YQ
authors.lastname: Long
authors.forename: Christophe
authors.initials: C
authors.lastname: Marchand
authors.forename: Yves
authors.initials: Y
authors.lastname: Pommier
authors.forename: Peter P
authors.initials: PP
authors.lastname: Roller
mesh_terms: D019281:Dimerization; D015195:Drug Design; D019427:HIV Integrase / Q000502:physiology*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D019428:HIV Integrase Inhibitors; D010455:Peptides; D019427:HIV Integrase