期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 26, 期 22, 页码 5896-5902出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2018.10.042
关键词
Antimetabolites; Pantothenate kinase inhibitors; PanK; Pantothenate kinase; Coenzyme A
资金
- Canadian Institute of Health Research
- South African National Research Foundation
Pantothenate kinase (PanK) catalyzes the transformation of pantothenate to 4'-phosphopantothenate, the first committed step in coenzyme A biosynthesis. While numerous pantothenate antimetabolites and PanK inhibitors have been reported for bacterial type I and type II PanKs, only a few weak inhibitors are known for bacterial type III PanK enzymes. Here, a series of pantothenate analogues were synthesized using convenient synthetic methodology. The compounds were exploited as small organic probes to compare the ligand preferences of the three different types of bacterial PanK. Overall, several new inhibitors and substrates were identified for each type of PanK.
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