Targeting bacterial topoisomerase I to meet the challenge of finding new antibiotics

Authors

Yuk-Ching Tse-Dinh, Department of Chemistry & Biochemistry, Florida International UniversityFollow

Date of this Version

1-1-2015

Document Type

Article

Rights

default

Abstract

Resistance of bacterial pathogens to current antibiotics has grown to be an urgent crisis. Approaches to overcome this challenge include identification of novel targets for discovery of new antibiotics. Bacterial topoisomerase I is present in all bacterial pathogens as a potential target for bactericidal topoisomerase poison inhibitors. Recent efforts have identified inhibitors of bacterial topoisomerase I with antibacterial activity. Additional research on the mode of action and binding site of these inhibitors would provide further validation of the target and establish that bacterial topoisomerase I is druggable. Bacterial topoisomerase I is a potentially high value target for discovery of new antibiotics. Demonstration of topoisomerase I as the cellular target of an antibacterial compound would provide proof-of-concept validation.

DOI

10.4155/fmc.14.157

Identifier

25875873

Comments

Pubmed Accepted Manuscript

Published in final edited form as: Future Med Chem. 2015 March ; 7(4): 459–471. doi:10.4155/fmc.14.157.

Recommended Citation

Tse-Dinh YC. Targeting bacterial topoisomerase I to meet the challenge of finding new antibiotics. Future Med Chem. 2015;7(4):459-71. doi: 10.4155/fmc.14.157. PMID: 25875873; PMCID: PMC4415981.