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Design and synthesis of dimeric HIV-1 integrase inhibitory peptides
Krzysztof Krajewski1, Ya-Qiu Long, Christophe Marchand
1Laboratory of Medicinal Chemistry, CCR, NCI-Frederick, NIH, Frederick, MD 21702, USA.
Bioorganic & Medicinal Chemistry Letters
|September 3, 2003
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.