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Tirandamycins from Streptomyces sp. 17944 inhibiting the parasite Brugia malayi asparagine tRNA synthetase. Org Lett 2011 Apr 15;13(8):2034-7

Date

03/17/2011

Pubmed ID

21405052

Pubmed Central ID

PMC3074013

DOI

10.1021/ol200420u

Scopus ID

2-s2.0-79955388062 (requires institutional sign-in at Scopus site)   56 Citations

Abstract

Lymphatic filariasis is caused by the parasitic nematodes Brugia malayi and Wuchereria bancrofti, and asparaginyl-tRNA synthetase (AsnRS) is considered an excellent antifilarial target. The discovery of three new tirandamycins (TAMs), TAM E (1), F (2), and G (3), along with TAM A (4) and B (5), from Streptomyces sp. 17944 was reported. Remarkably, 5 selectively inhibits the B. malayi AsnRS and efficiently kills the adult B. malayi parasite, representing a new lead scaffold to discover and develop antifilarial drugs.

Author List

Yu Z, Vodanovic-Jankovic S, Ledeboer N, Huang SX, Rajski SR, Kron M, Shen B

Authors

Michael Kron MD Director, Professor in the Medicine department at Medical College of Wisconsin
Nathan A. Ledeboer PhD Vice Chair, Professor in the Pathology department at Medical College of Wisconsin




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

Aminoglycosides
Animals
Anti-Bacterial Agents
Aspartate-tRNA Ligase
Brugia malayi
Enzyme Inhibitors
Models, Molecular
Molecular Structure
RNA, Transfer, Amino Acyl
Streptomyces