SYNTHESIS OF SOME PEPTIDES CORRESPONDING TO THE ACTIVE REGION OF RANTES FOR CHEMOTAXIS AND EVALUATION OF THEIR ANTI-HUMAN IMMUNODEFICIENCY VIRUS-1 ACTIVITY

Abstract

Five peptides corresponding to the amino-terminal sequence of RANTES (regulated upon activation, normal T-cell expressed and sereted), 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.