Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity.

Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Research Abstract Details 

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Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Abstract Text:

Shuai Chen,Xuemei Zhao,Jinzhi Tan,Hong Lu,Zhi Qi,Qiang Huang,Xianzhuo Zeng,Mingjun Zhang,Shibo Jiang,Hualiang Jiang,Long Yu,

Cyclophilin A acts as protein folding chaperones and intracellular transports in many cellular processes. Previous studies have shown that cyclophilin A can interact with HIV-1 (human immunodeficiency virus type 1) gag protein and enhance viral infectivity. Many cyclophilin A inhibitors such as cyclosporin A can inhibit HIV-1 replication in vitro. Here, we report a structure-based identification of novel non-peptidic cyclophilin A inhibitors as anti-HIV lead compounds. Following a computer-aided virtual screening and subsequent surface plasmon resonance (SPR) analysis, 12 low molecular weight cyclophilin A ligands were selected for further evaluation of their in vitro inhibition of peptidyl-prolyl cis-trans isomerase (PPIase) activity of cyclophilin A and HIV-1 replication. Five of these compounds (FD5, FD8, FD9, FD10 and FD12) exhibited inhibition against both PPIase activity and HIV-1 infection. These active compounds will be used as leads for structure and activity relationship (SAR) and optimization studies in order to design more effective anti-HIV-1 therapeutics, and as probes for investigating the effect of cyclophilins on HIV-1 replication.

Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Publishing Authors By Initials

S Chen,X Zhao,J Tan,H Lu,Z Qi,Q Huang,X Zeng,M Zhang,S Jiang,H Jiang,L Yu,

For similar biological phenomena, cell phenomena, and immunity: biological phenomena: microbiologic phenomena: viral physiology: virus replication research abstracts see: biological phenomena, cell phenomena, and immunity: biological phenomena: microbiologic phenomena: viral physiology: virus replication research

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Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: European journal of pharmacology

VOLUME: 565

Page Numbers: 54-9

Journal Abbreviation: Eur. J. Pharmacol.

ISSN: 0014-2999

DAY: 24

MONTH: 03

YEAR: 2007

Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 1254354

Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Keywords Mesh Terms:

KEYWORDS: Virus Replication

MESH TERMS: drug effects

Chemical & Substance for Abstract: Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity. Information

Substance Name: Peptidylprolyl Isomerase

Registry Number: EC 5.2.1.8

Grant and Affiliation Information for Structure-based identification of small molecule compounds targeting cell cyclophilin A with anti-HIV-1 activity.

AFFILIATION: State Key Laboratory of Genetic Engineering, Institute of Genetics, School of Life Sciences, Fudan University, People's Republic of China.

Country: Netherlands

AGENCY: United States NIAID

GRANT: AI46221

ACRONYM: AI

MEDLINETA: Eur J Pharmacol

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