Synthesis and biological evaluation of phosphonic and thiophosphoric acid (cas 13598-51-1) derivatives of lysophosphatidic acid
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Add time:08/26/2019 Source:sciencedirect.com
Using an N-oleoyl ethanolamide scaffold, a series of phosphate polar head group analogues of LPA comprised of various α-substituted phosphonates and thiophosphates was prepared. In a broken cell GTP[γ35S] binding assay, agonist activity was evaluated at the three LPA receptors of the endothelial differentiation gene (Edg) family. This study has resulted in the discovery of a nonhydrolyzable LPA1-selective agonist (11). Additionally, thiophosphate 19 bears an isosteric phosphate mimetic that confers agonism at the LPA1 receptor but not LPA2.
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