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Design and synthesis of dimeric HIV-1 integrase inhibitory peptides

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
13
Issue
19
Identifiers
DOI: 10.1016/s0960-894x(03)00679-6
Disciplines
  • Design

Abstract

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 μM, for 3′-end processing and strand transfer, respectively.

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