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4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862
Institute of Medicinal Biotechnology, Peking Union Medical College, Chinese Academy of Medical Sciences, Tiantanxili No.1, Beijing 100050, China
National Institute of Biological Sciences, 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, China
* Author to whom correspondence should be addressed.
Received: 31 October 2012; in revised form: 14 December 2012 / Accepted: 18 December 2012 / Published: 27 December 2012
Abstract: 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.
Keywords: Streptomyces albosporus; structure elucidation; HIV-1 protease inhibitor
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Liu, X.; Gan, M.; Dong, B.; Zhang, T.; Li, Y.; Zhang, Y.; Fan, X.; Wu, Y.; Bai, S.; Chen, M.; Yu, L.; Tao, P.; Jiang, W.; Si, S. 4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862. Molecules 2013, 18, 236-243.
Liu X, Gan M, Dong B, Zhang T, Li Y, Zhang Y, Fan X, Wu Y, Bai S, Chen M, Yu L, Tao P, Jiang W, Si S. 4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862. Molecules. 2013; 18(1):236-243.
Liu, Xiao; Gan, Maoluo; Dong, Biao; Zhang, Tian; Li, Yongzhen; Zhang, Yuqin; Fan, Xiuyong; Wu, Yexiang; Bai, Shuoke; Chen, Minghua; Yu, Liyan; Tao, Peizhen; Jiang, Wei; Si, Shuyi. 2013. "4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862." Molecules 18, no. 1: 236-243.