| Literature DB >> 32031795 |
Bin Zhou1,2, Gauri Shetye2, Yang Yu1, Bernard D Santarsiero1,3, Larry L Klein1,2, Cele Abad-Zapatero2,3, Nina M Wolf2, Jinhua Cheng4,5, Yingyu Jin4, Hanki Lee4, Joo-Won Suh4, Hyun Lee1,2,3, Jonathan Bisson1,2, James B McAlpine1,2, Shao-Nong Chen1,2, Sang-Hyun Cho1,2, Scott G Franzblau1,2, Guido F Pauli1,2.
Abstract
This study represents a systematic chemical and biological study of the rufomycin (RUF) class of cyclic heptapeptides, which our anti-TB drug discovery efforts have identified as potentially promising anti-TB agents that newly target the caseinolytic protein C1, ClpC1. Eight new RUF analogues, rufomycins NBZ1-NBZ8 (1-8), as well as five known peptides (9-13) were isolated and characterized from the Streptomyces atratus strain MJM3502. Advanced Marfey's and X-ray crystallographic analysis led to the assignment of the absolute configuration of the RUFs. Several isolates exhibited potent activity against both pathogens M. tuberculosis H37Rv and M. abscessus, paired with favorable selectivity (selectivity index >60), which collectively underscores the promise of the rufomycins as potential anti-TB drug leads.Entities:
Year: 2020 PMID： 32031795 PMCID： PMC7384767 DOI： 10.1021/acs.jnatprod.9b01095
Source DB: PubMed Journal: J Nat Prod ISSN： 0163-3864 Impact factor: 4.050