Thiolactomycin-Based Inhibitors of Bacterial β-Ketoacyl-ACP Synthases with in Vivo Activity
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چکیده
منابع مشابه
Platensimycin Activity against Mycobacterial β-Ketoacyl-ACP Synthases
BACKGROUND There is an urgent need for the discovery and development of new drugs against Mycobacterium tuberculosis, the causative agent of tuberculosis, especially due to the recent emergence of multi-drug and extensively-drug resistant strains. Herein, we have examined the susceptibility of mycobacteria to the natural product platensimycin. METHODS AND FINDINGS We have demonstrated that pl...
متن کاملReview of Platensimycin and Platencin: Inhibitors of β-Ketoacyl-acyl Carrier Protein (ACP) Synthase III (FabH).
Platensimycin and platencin were successively discovered from the strain Streptomyces platensis through systematic screening. These natural products have been defined as promising agents for fighting multidrug resistance in bacteria by targeting type II fatty acid synthesis with slightly different mechanisms. Bioactivity studies have shown that platensimycin and platencin offer great potential ...
متن کاملShewanella oneidensis FabB: A β-ketoacyl-ACP Synthase That Works with C16:1-ACP
It is established that Escherichia coli β-ketoacyl-ACP synthase (KAS) I (encoded by EcfabB) is the primary, if not exclusive, factor for elongation of the cis-3-decenoyl-ACP (C10:1-ACP) but not effective with C16:1- or longer-chain-ACPs. To test the extent to which these features apply to KAS I proteins in other species, in this study, we examined the physiological role of FabB in Shewanella on...
متن کاملThe effect of thiolactomycin analogues on fatty acid synthesis in peas (Pisum sativum cv. Onward).
Thiolactomycin is an inhibitor of type I1 dissociable fatty acid synthases from plants and bacteria [ 1 1. The three P-ketoacyl acyl carrier protein (ACP) synthases in peas are all inhibited by thiolactomycin [2]. Condensing enzyme I1 (KAS II), which catalyses the elongation of palmitoyl-ACP to stearoyl-ACP is the most sensitive and the short chain condensing enzyme (KAS III), which catalyses t...
متن کاملNovel inhibitors of the condensing enzymes of the type II fatty acid synthase of pea (Pisum sativum).
The type II fatty acid synthases (FASs) of higher plants (and Escherichia coli) contain three condensing enzymes called beta-ketoacyl-ACP synthases (KAS), where ACP is acyl-carrier-protein. We have used novel derivatives of the antibiotic thiolactomycin to inhibit these enzymes. Overall de novo fatty acid biosynthesis was measured using [1-(14)C]acetate substrate and chloroplast preparations fr...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2016
ISSN: 0022-2623,1520-4804
DOI: 10.1021/acs.jmedchem.6b00236