Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.
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.
Krajewski
Krzysztof
K
Laboratory of Medicinal Chemistry, CCR, NCI-Frederick, NIH, Frederick, MD 21702, USA.
Long
Ya-Qiu
YQ
Marchand
Christophe
C
Pommier
Yves
Y
Roller
Peter P
PP
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
D019428:HIV Integrase Inhibitors; D010455:Peptides; D019427:HIV Integrase