New WS9326A congeners from Streptomyces sp. 9078 inhibiting Brugia malayi asparaginyl-tRNA synthetase. Org Lett 2012 Sep 21;14(18):4946-9
Date
09/13/2012Pubmed ID
22967068Pubmed Central ID
PMC3460372DOI
10.1021/ol302298kScopus ID
2-s2.0-84868245096 (requires institutional sign-in at Scopus site) 49 CitationsAbstract
Lymphatic filariasis is caused by the Brugia malayi parasite. Three new congeners of the depsipeptide WS9326A (1), WS9326C (2), WS9326D (3), and WS9326E (4), were isolated from Streptomyces sp. 9078 by using a B. malayi asparaginyl-tRNA synthetase (BmAsnRS) inhibition assay. WS9326D specifically inhibits the BmAsnRS, kills the adult B. malayi parasite, and does not exhibit significant general cytotoxicity to human hepatic cells, representing a new lead scaffold for antifilarial drug discovery.
Author List
Yu Z, Vodanovic-Jankovic S, Kron M, Shen BAuthor
Michael Kron MD Director, Professor in the Medicine department at Medical College of WisconsinMESH terms used to index this publication - Major topics in bold
AnimalsAspartate-tRNA Ligase
Brugia malayi
Filariasis
Hepatocytes
Humans
Lactones
Molecular Structure
Peptides, Cyclic
RNA, Transfer, Amino Acyl
Stereoisomerism
Streptomyces