Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket

doi:10.1007/s00726-012-1394-8

CORC > 北京大学 > 化学与分子工程学院

	Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket
	Bai, Yu ; Xue, Huifang ; Wang, Kun ; Cai, Lifeng ; Qiu, Jiayin ; Bi, Shuangyu ; Lai, Luhua ; Cheng, Maosheng ; Liu, Shuwen ; Liu, Keliang
刊名	氨基酸
	2013
关键词	HIV-1 Gp41 Peptide Six-helix bundle Covalent inhibitor VIRUS TYPE-1 GP41 COILED-COIL ANTIRETROVIRAL ACTIVITY BIOMIMETIC CATALYSIS AMINOACYL-TRANSFER PEPTIDE INHIBITOR 6-HELICAL BUNDLE ATOMIC-STRUCTURE CORE STRUCTURE ACYL TRANSFER
DOI	10.1007/s00726-012-1394-8
英文摘要	Covalent inhibitors form covalent adducts with their target, thus permanently inhibiting a physiological process. Peptide fusion inhibitors, such as T20 (Fuzeon, enfuvirtide) and C34, interact with the N-terminal heptad repeat of human immunodeficiency virus type 1 (HIV-1) gp41 glycoprotein to form an inactive hetero six-helix bundle (6-HB) to prevent HIV-1 infection of host cells. A covalent strategy was applied to peptide fusion inhibitor design by introducing a thioester group into C34-like peptide. The modified peptide maintains the specific interaction with its target N36. After the 6-HB formation, a covalent bond between C- and N-peptides was formed by an inter-helical acyl transfer reaction, as characterized by various biophysical and biochemical methods. The covalent reaction between the reactive C-peptide fusion inhibitor and its N-peptide target is highly selective, and the reaction greatly increases the thermostability of the 6-HB. The modified peptide maintains high potency against HIV-1-mediated cell-cell fusion and infection.; http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000313794600038&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=8e1609b174ce4e31116a60747a720701 ; Biochemistry & Molecular Biology; SCI(E); 6; ARTICLE; 2; 701-713; 44
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/236765]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Bai, Yu,Xue, Huifang,Wang, Kun,et al. Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket[J]. 氨基酸,2013.
APA	Bai, Yu.,Xue, Huifang.,Wang, Kun.,Cai, Lifeng.,Qiu, Jiayin.,...&Liu, Keliang.(2013).Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket.氨基酸.
MLA	Bai, Yu,et al."Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket".氨基酸 (2013).