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-NH2 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 IC50 values of 5.3 and 6.5 μM, for 3′-end processing and strand transfer, respectively.