4862F, a new inhibitor of HIV-1 protease, from the culture of Streptomyces I03A-04862.

Research paper by Xiao X Liu, Maoluo M Gan, Biao B Dong, Tian T Zhang, Yongzhen Y Li, Yuqin Y Zhang, Xiuyong X Fan, Yexiang Y Wu, Shuoke S Bai, Minghua M Chen, Liyan L Yu, Peizhen P Tao, Wei W Jiang, Shuyi S Si

Indexed on: 29 Dec '12Published on: 29 Dec '12Published in: Molecules (Basel, Switzerland)


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.