ArticleBioorganic & medicinal chemistry2014
Reaction intermediate analogues as bisubstrate inhibitors of pantothenate synthetase.
Article in Bioorganic & medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 22 citations in OpenAlex.
- Review
- TargetingACS infectious diseases · 2021Article
- Inhibitors of pantothenate synthetase ofRSC advances · 2020Review
- Vitamin in the Crosshairs: Targeting Pantothenate and Coenzyme A Biosynthesis for New Antituberculosis Agents.Frontiers in cellular and infection microbiology · 2020Review
- Targeting adenylate-forming enzymes with designed sulfonyladenosine inhibitors.The Journal of antibiotics · 2019Review
- Opposing reactions in coenzyme A metabolism sensitizeScience (New York, N.Y.) · 2019Article
- Validation of CoaBC as a Bactericidal Target in the Coenzyme A Pathway of Mycobacterium tuberculosis.ACS infectious diseases · 2016Article
- Design, synthesis, and biological evaluation of α-hydroxyacyl-AMS inhibitors of amino acid adenylation enzymes.Bioorganic & medicinal chemistry letters · 2016Article
- Improved Synthesis of Biotinol-5'-AMP: Implications for Antibacterial Discovery.ACS medicinal chemistry letters · 2015Article
- The application of tetracyclineregulated gene expression systems in the validation of novel drug targets in Mycobacterium tuberculosis.Frontiers in microbiology · 2015Review
- Future target-based drug discovery for tuberculosis?Tuberculosis (Edinburgh, Scotland) · 2014Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
Abstract
The biosynthesis of pantothenate, the core of coenzyme A (CoA), has been considered an attractive target for the development of antimicrobial agents since this pathway is essential in prokaryotes, but absent in mammals. Pantothenate synthetase, encoded by the gene panC, catalyzes the final condensation of pantoic acid with β-alanine to afford pantothenate via an intermediate pantoyl adenylate. We describe the synthesis and biochemical characterization of five PanC inhibitors that mimic the intermediate pantoyl adenylate. These inhibitors are competitive inhibitors with respect to pantoic acid and possess submicromolar to micromolar inhibition constants. The observed SAR is rationalized through molecular docking studies based on the reported co-crystal structure of 1a with PanC. Finally, whole cell activity is assessed against wild-type Mtb as well as a PanC knockdown strain where PanC is depleted to less than 5% of wild-type levels.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.