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Five peptides corresponding to the amino-terminal sequence of RANTES (regulated upon activation, normal T-cell expressed and secreted), which is known to be the critical region for chemotaxis, were synthesized, and their anti-human immunodeficiency virus (HIV)-1 activity was examined to obtain a lead compound useful for the development of chemokine receptor-directed anti-HIV-1 drugs. A decapeptide corresponding to positions 1-10 [Ac-(10Ala-RANTES 1-10)-NH2] showed significant anti-HIV-1 activity. Ac-(10Ala, 11Ala-RANTES 5-14)-NH2 was also active, but less potent than the former. Other peptides corresponding to the positions 6-14, 7-14, and 8-14 did not show anti-HIV-1 activity. These results indicate that the sequence 1-10 of RANTES is important for the anti-HIV-1 effect.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Synthesis of Some Peptides Corresponding to the Active Region of Rantes for Chemotaxis and Evaluation of Their Anti-human Immunodeficiency Virus-1 Activity.