title: 4862F, a new inhibitor of HIV-1 protease, from the culture of Streptomyces I03A-04862.
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.
authors.affiliation: Institute of Medicinal Biotechnology, Peking Union Medical College, Chinese Academy of Medical Sciences, Tiantanxili No.1, Beijing 100050, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Liu
authors.forename: Maoluo
authors.initials: M
authors.lastname: Gan
authors.forename: Biao
authors.initials: B
authors.lastname: Dong
authors.forename: Tian
authors.initials: T
authors.lastname: Zhang
authors.forename: Yongzhen
authors.initials: Y
authors.lastname: Li
authors.forename: Yuqin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xiuyong
authors.initials: X
authors.lastname: Fan
authors.forename: Yexiang
authors.initials: Y
authors.lastname: Wu
authors.forename: Shuoke
authors.initials: S
authors.lastname: Bai
authors.forename: Minghua
authors.initials: M
authors.lastname: Chen
authors.forename: Liyan
authors.initials: L
authors.lastname: Yu
authors.forename: Peizhen
authors.initials: P
authors.lastname: Tao
authors.forename: Wei
authors.initials: W
authors.lastname: Jiang
authors.forename: Shuyi
authors.initials: S
authors.lastname: Si
mesh_terms: D000596:Amino Acids / Q000032:analysis; D002851:Chromatography, High Pressure Liquid; D005285:Fermentation; D017320:HIV Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology*; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology*; D013302:Streptomyces / Q000378:metabolism*
chemical_list: C581495:4862F peptide; D000596:Amino Acids; D017320:HIV Protease Inhibitors; D009842:Oligopeptides; D010455:Peptides