源自CC趋化因子RANTES部分氨基酸序列的抗HIV-1肽。在激活时受到调节，由正常T细胞表达和分泌。

Anti-HIV-1 peptides derived from partial amino acid sequences of CC-chemokine RANTES. Regulated upon activation, normal T-cell expressed and secreted.

作者信息

Nishiyama Yasuhiro, Murakami Tsutomu, Shikama Suguru, Kurita Keisuke, Yamamoto Naoki

机构信息

Chemical Immunology and Therapeutics Research Center, Department of Pathology and Laboratory Medicine, University of Texas-Houston Medical School, 77030, USA.

出版信息

Bioorg Med Chem. 2002 Dec;10(12):4113-7. doi: 10.1016/s0968-0896(02)00271-7.

DOI:10.1016/s0968-0896(02)00271-7

PMID:12413865

Abstract

Fifteen acetyl-peptide-amides with partial amino acid sequences of RANTES (regulated upon activation, normal T-cell expressed and secreted), all Cys residues of which were substituted by Ala, were synthesized, and screened for anti-HIV-1 activity. Peptides corresponding to 1-10, 37-46, and 57-68 showed marked activity against CC-chemokine receptor 5-using HIV-1(JR-CSF) (% inhibition at 100 nM 69, 82, 76%, respectively). The results indicate that multiple regions, including the N-terminal part responsible for chemotactic activity, are involved in anti-HIV-1 activity of RANTES, yielding possible lead compounds for anti-HIV-1 agents.

摘要

合成了15种具有RANTES（活化时调节、正常T细胞表达和分泌）部分氨基酸序列的乙酰化肽酰胺，其中所有半胱氨酸残基均被丙氨酸取代，并筛选了其抗HIV-1活性。对应于1-10、37-46和57-68的肽对使用CC趋化因子受体5的HIV-1（JR-CSF）显示出显著活性（在100 nM时的抑制率分别为69%、82%、76%）。结果表明，包括负责趋化活性的N端部分在内的多个区域参与了RANTES的抗HIV-1活性，从而产生了可能的抗HIV-1药物先导化合物。