4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862

Autor: Peizhen Tao, Wei Jiang, Liyan Yu, Minghua Chen, Shuoke Bai, Yexiang Wu, Xiuyong Fan, Yuqin Zhang, Yongzhen Li, Tian Zhang, Biao Dong, Maoluo Gan, Xiao Liu, Shuyi Si
Jazyk: angličtina
Rok vydání: 2012
Předmět:
Zdroj: Molecules, Vol 18, Iss 1, Pp 236-243 (2012)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules18010236
Popis: We have isolated an extraordinary pentapeptide, called 4862F, from the culture broth of Streptomyces albosporus I03A-04862 by Diaion HP-20 macroporous adsorbent resin column, ODS-A and Sephadex LH-20 chromatography, followed by preparative HPLC. This peptide shows inhibitory activity against HIV-1 protease. The structure was elucidated by spectroscopic approaches, including ESI-MS and various NMR methods. Absolute configuration of the amino acid residues in 4862F was defined using Marfey’s method, and the structure was identified as N,N,N-(trimethylated)-Tyr-L-Leu-L-Val-L-Leu-(dehydrated)-His. The peptide 4862F displays inhibitory activity against HIV-1 protease, with IC50 values of 15.26 nM, using a fluorescence-based assay.
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