Bacterial Cytological Profiling Identifies Rhodanine-Containing PAINS Analogs as Specific Inhibitors of Escherichia coli Thymidylate Kinase In Vivo-Reference-Cited by-同舟云学术

Bacterial Cytological Profiling Identifies Rhodanine-Containing PAINS Analogs as Specific Inhibitors of Escherichia coli Thymidylate Kinase In Vivo

Published:2021-09-08 Issue:19 Volume:203 Page:
ISSN:0021-9193
Container-title:Journal of Bacteriology
language:en
Short-container-title:J Bacteriol

Author:

Montaño Elizabeth T.¹,Nideffer Jason F.¹,Sugie Joseph¹,Enustun Eray¹,Shapiro Adam B.²^ORCID,Tsunemoto Hannah¹,Derman Alan I.¹,Pogliano Kit¹,Pogliano Joe¹

Affiliation:

1. Division of Biological Sciences, University of California—San Diego, La Jolla, California, USA

2. Entasis Therapeutics, Gatehouse Park BioHub, Waltham, Massachusetts, USA

Abstract

We demonstrate that bacterial cytological profiling is a powerful tool for directing antibiotic discovery efforts because it can be used to determine the specificity of an antibiotic’s in vivo mechanism of action. By assaying analogs of PAINS, molecules that are notoriously intractable and nonspecific, we (surprisingly) identify molecules with specific activity against E. coli thymidylate kinase.

Funder

Foundation for the National Institutes of Health

Publisher

American Society for Microbiology

Subject

Molecular Biology,Microbiology

Link

https://journals.asm.org/doi/pdf/10.1128/JB.00105-21

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