Synthesis of some peptides corresponding to the active region of RANTES for chemotaxis and evaluation of their anti-human immunodeficiency virus-1 activity.
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.
Nishiyama
Y
Y
Department of Industrial Chemistry, Faculty of Engineering, Seikei University, Tokyo, Japan.
Murakami
T
T
Kurita
K
K
Yamamoto
N
N
D000595:Amino Acid Sequence; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002478:Cells, Cultured; D018946:Chemokine CCL5 / Q000737:chemistry*; D002633:Chemotaxis / Q000187:drug effects*; D004797:Enzyme-Linked Immunosorbent Assay; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D011994:Recombinant Proteins / Q000737:chemistry; D016339:Spectrometry, Mass, Fast Atom Bombardment
D019380:Anti-HIV Agents; D018946:Chemokine CCL5; D010455:Peptides; D011994:Recombinant Proteins