Open AccessArticle
4862F, a New Inhibitor of HIV-1 Protease, from the Culture of Streptomyces I03A-04862
by
Xiao Liu, Maoluo Gan, Biao Dong, Tian Zhang, Yongzhen Li, Yuqin Zhang, Xiuyong Fan, Yexiang Wu, Shuoke Bai, Minghua Chen, Liyan Yu, Peizhen Tao, Wei Jiang and Shuyi Si
Cited by 15 | Viewed by 5110
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
[...] Read more.
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 IC
50 values of 15.26 nM, using a fluorescence-based assay.
Full article
►▼
Show Figures
