军事医学2012，Vol.36Issue(5)：332-336,5.
新型HIV-1gp41融合抑制剂CP32M的构效关系研究
Structure-activity relationships of novel HIV-1 gp41 fusion peptide CP32M
摘要
Abstract
Objective To probe the effect of length, electric charge and fragment replacement of the key domain VEWNEMT and other residues in CP32M on its inhibitory activity to HIV-1 gp41 fusion. Methods Based on CP32M, a series of polypeptides of varied lengths and with electric charges and other functional fragments were designed and synthe-sized. The anti-HIV-1 activities were tested using HIV-1 ⅢB virus, and interaction with N36 was determined by circular di-chroism spectrum and size-exclusion HPLC. Results Truncation and partial residue replacement in the fragment VEWNEMT or introduction of i to i + 4 Glu-Lys ion pair interaction in the center or at C terminus of CP32M resulted in a decrease in the anti-HIV-1 activity of gp41 and the content of a-helix. The substitution of VEWNEMT by the fragment NEKDLLE derived from C terminus of C34 and a gpl20 binding peptide RINNIPWSEAM rescued the inhibitory activity. Conclusion VEWNEMT is the key fragment for CP32M, and residues VE and MT are crucial functional amino acids. The replacement of VEWNEMT by other functional domain retains high anti-HIV-1 activity and high content of helical structure, suggesting that this fragment contains a commons binding area.关键词
HIV-1/HIV包膜蛋白质gp41/多肽/CP32M/构效关系Key words
HIV-1/ HIV envolope protein gp41/ polypeptide/ CP32M/ structure-activity relationship分类
医药卫生引用本文复制引用
王孝花,成健伟,朱卫国,董铭心,种辉辉,何玉先,戴秋云..新型HIV-1gp41融合抑制剂CP32M的构效关系研究[J].军事医学,2012,36(5):332-336,5.基金项目
国家自然科学基金资助项目(81072676) （81072676）
国家科技重大专项资助项目(2009ZX09103-628) （2009ZX09103-628）
