Anti-HIV-1 Peptide Derivatives Based on the HIV-1 Co-receptor CXCR4 (pages 1668–1672)
Dr. Chie Hashimoto, Dr. Wataru Nomura, Dr. Tetsuo Narumi, Dr. Masayuki Fujino, Dr. Hiroshi Tsutsumi, Masaki Haseyama, Prof. Naoki Yamamoto, Dr. Tsutomu Murakami and Prof. Hirokazu Tamamura
Article first published online: 23 AUG 2013 | DOI: 10.1002/cmdc.201300289
Several peptide derivatives of CXCR4 extracellular domains were synthesized and evaluated for anti-HIV-1 activity. The 39-mer N-terminal region (NT) was divided into three fragments with 10-mer overlapping sites, and these linear peptides were synthesized. The peptide containing Met 1–Asp 20 shows significant anti-HIV-1 activity. Extracellular loops 1 and 2 (ECL1 and 2) were mimicked by cyclic peptides, synthesized by chemoselective cyclization. Both show higher anti-HIV-1 activity than their linear counterparts. These results show that Met 1–Asp 20 on the NT and cyclic peptides of ECL1 and ECL2 are potent anti-HIV-1 drug candidates.