Design of highly potent HIV fusion inhibitors based on artificial peptide sequences

Weiguo Shi; Lifeng Cai; Lu Lu; Chao Wang; Kun Wang; Liang Xu; Sha Zhang; Han Han; Xifeng Jiang; Baohua Zheng; Shibo Jiang; Keliang Liu

doi:10.1039/C2CC35973A

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Chemical Communications

Issue 94, 2012

Urgent high quality communications from across the chemical sciences.

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Design of highly potent HIV fusion inhibitors based on artificial peptide sequences

Weiguo Shi,^a Lifeng Cai,^a Lu Lu,^b Chao Wang,^a Kun Wang,^a Liang Xu,^a Sha Zhang,^a Han Han,^a Xifeng Jiang,^a Baohua Zheng,^a Shibo Jiang*^b and Keliang Liu*^a

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Department of Medicinal Chemistry, Beijing Institute of Pharmacology & Toxicology, 27 Taiping Rd, Haidian District, China
E-mail: keliangliu55@126.com ;
Fax: +86-10-68211656

Key Lab of Medical Molecular Virology (Ministries of Education and Health), Shanghai Medical College and Institute of Medical Microbiology, Fudan University 130 Dong An Road, Xuhui District, China
E-mail: shibojiang@fudan.edu.cn ;
Fax: +86-21-54237465

Chem. Commun., 2012,48, 11579-11581

DOI: 10.1039/C2CC35973A
Received 17 Aug 2012, Accepted 12 Oct 2012
First published online 12 Oct 2012

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Specific interactions were introduced between an artificial heptad repeat peptide template and HIV-1 gp41 for fusion inhibitor design, using a structure based rational design strategy. The designed peptides are nonhomologous with naturally occurring peptide and protein sequences, specifically interact with HIV-1 gp41, and show strong anti-HIV activity.

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