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• W2092922189 endingPage "776" @default.
• W2092922189 startingPage "769" @default.
• W2092922189 abstract "Autotaxin (ATX) is a member of the ecto-nucleotide pyrophosphatase/phosphodiesterase (NPP) family and is a lysophospholipase D that cleaves the choline headgroup from lysophosphatidylcholine to generate the bioactive lipid lysophosphatidic acid (LPA). Enhanced expression of ATX and specific receptors for LPA in numerous cancer cell types has created an interest in studying ATX as a potential chemotherapeutic target. Likewise, ATX has been linked to several additional human diseases including multiple sclerosis, diabetes, obesity, neuropathic pain, and Alzheimer’s disease. ATX inhibitors reported to date consist of metal ion chelators, lipid-like product analogs, and non-lipid small molecules. In the current research, we examined the pharmacology of the best of our previously reported non-lipid small molecule inhibitors. Here, these six inhibitors were studied utilizing the synthetic fluorescent lysophospholipid substrate FS-3, the nucleotide substrate pNP-TMP and the endogenous substrate LPC (16:0). All six compounds inhibited FS-3 hydrolysis ⩾50%, whereas only three inhibited the hydrolysis of pNP-TMP to this degree. None of the six compounds blocked LPC 16:0 hydrolysis within the desired 50% inhibition range. The most potent analog (5, H2L 7905958) displayed an IC50 of 1.6 μM (Ki = 1.9 μM, competitive inhibition) with respect to ATX-mediated FS-3 hydrolysis and an IC50 of 1.2 μM (Ki=Ki′=6.5μM, non-competitive inhibition) against ATX-mediated pNP-TMP hydrolysis. All six inhibitors were specific for ATX as they were without affect on two additional lipid preferring NPP isoforms." @default.
• W2092922189 created "2016-06-24" @default.
• W2092922189 creator A5011729936 @default.
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• W2092922189 creator A5058935164 @default.
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• W2092922189 date "2010-01-01" @default.
• W2092922189 modified "2023-10-04" @default.
• W2092922189 title "Characterization of non-lipid autotaxin inhibitors" @default.
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• W2092922189 doi "https://doi.org/10.1016/j.bmc.2009.11.056" @default.
• W2092922189 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20005724" @default.
• W2092922189 hasPublicationYear "2010" @default.
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