A Fluorescence-Based Assay for Identification of Bacterial Topoisomerase I Poisons

Thirunavukkarasu Annamalai; Bokun Cheng; Neelam Keswani; Yuk-Ching Tse-Dinh

doi:10.1007/978-1-4939-7459-7_18

A Fluorescence-Based Assay for Identification of Bacterial Topoisomerase I Poisons

Methods Mol Biol. 2018:1703:259-268. doi: 10.1007/978-1-4939-7459-7_18.

Authors

Thirunavukkarasu Annamalai^{1

2}, Bokun Cheng³, Neelam Keswani^{1

2}, Yuk-Ching Tse-Dinh^{4

5}

Affiliations

¹ Department of Chemistry and Biochemistry, Florida International University, Miami, FL, USA.
² Biomolecular Sciences Institute, Florida International University, Miami, FL, USA.
³ Department of Pediatrics, Albert Einstein College of Medicine, Bronx, NY, USA.
⁴ Department of Chemistry and Biochemistry, Florida International University, Miami, FL, USA. yukching.tsedinh@fiu.edu.
⁵ Biomolecular Sciences Institute, Florida International University, Miami, FL, USA. yukching.tsedinh@fiu.edu.

PMID: 29177747
DOI: 10.1007/978-1-4939-7459-7_18

Abstract

Bacterial Topoisomerase I is a potential target for the identification of novel topoisomerase poison inhibitors that could provide leads for a new class of antibacterial compounds. Here we describe in detail a fluorescence-based cleavage assay that is successfully used in HTS for the discovery of bacterial topoisomerase Ι poisons.

Keywords: Bacterial topoisomerase I; Fluorescence-based assay; High-throughput screening; Topoisomerase I poisons.

MeSH terms

DNA Topoisomerases, Type I / metabolism*
DNA, Bacterial / chemistry
Drug Discovery
Escherichia coli / drug effects
Escherichia coli / enzymology*
Fluorescence
Nucleic Acid Conformation
Structure-Activity Relationship
Topoisomerase I Inhibitors / chemical synthesis*
Topoisomerase I Inhibitors / chemistry
Topoisomerase I Inhibitors / pharmacology
Yersinia pestis / drug effects
Yersinia pestis / enzymology*

Substances

DNA, Bacterial
Topoisomerase I Inhibitors
DNA Topoisomerases, Type I

Abstract

MeSH terms

Substances

Grants and funding