Antimycobacterial Rufomycin Analogues from Streptomyces atratus Strain MJM3502
| Autor: | James B. McAlpine, Guido F. Pauli, Shao-Nong Chen, Hyun Lee, Joo-Won Suh, Cele Abad-Zapatero, Nina M. Wolf, Sang-Hyun Cho, Bin Zhou, Scott G. Franzblau, Gauri Shetye, Jonathan Bisson, Hanki Lee, Yang Yu, Jinhua Cheng, Larry L. Klein, Ying-Yu Jin, Bernard D. Santarsiero |
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| Rok vydání: | 2020 |
| Předmět: |
medicine.drug_class
Stereochemistry Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Crystallography X-Ray Antimycobacterial 01 natural sciences Article Analytical Chemistry Drug Discovery medicine Streptomyces atratus Uncategorized Pharmacology Molecular Structure Strain (chemistry) 010405 organic chemistry Extramural Drug discovery Chemistry Organic Chemistry Absolute configuration Mycobacterium tuberculosis Streptomyces 0104 chemical sciences 010404 medicinal & biomolecular chemistry Complementary and alternative medicine Molecular Medicine Oligopeptides |
| Zdroj: | J Nat Prod |
| ISSN: | 1520-6025 0163-3864 |
| DOI: | 10.1021/acs.jnatprod.9b01095 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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