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New WS9326A congeners from Streptomyces sp. 9078 inhibiting Brugia malayi asparaginyl-tRNA synthetase. Org Lett 2012 Sep 21;14(18):4946-9

Date

09/13/2012

Pubmed ID

22967068

Pubmed Central ID

PMC3460372

DOI

10.1021/ol302298k

Abstract

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 B

Author

Michael Kron MD Director, Professor in the Medicine department at Medical College of Wisconsin




MESH terms used to index this publication - Major topics in bold

Animals
Aspartate-tRNA Ligase
Brugia malayi
Filariasis
Hepatocytes
Humans
Lactones
Molecular Structure
Peptides, Cyclic
RNA, Transfer, Amino Acyl
Stereoisomerism
Streptomyces
jenkins-FCD Prod-410 e9586552fe7f53c71f7923aa6e27aeabbd3c2473