Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling
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- 作者：John Gatfield ; john.gatfield@actelion.com" class="auth_mail ; Lucile Monnier ; Rolf Studer ; Martin H. Bolli ; Beat Steiner ; Oliver Nayler
- 关键词：BSA ; bovine serum albumin ; CHO ; Chinese hamster ovary ; CRC ; concentration&ndash ; response curve ; EC50 ; half maximimal excitatory concentration ; Emax ; maximal efficacy versus a defined control ; FBS ; fetal bovine serum ; GPCR ; G protein coupled receptor ; GRK ; GPCR related kinase ; HUVEC ; human umbilical vein endothelial cells ; PBS ; phosphate buffered saline ; S1P ; sphingosine-1-phosphate ; S1PR ; sphingosine-1-phosphate receptor ; SPL ; S1P lyase ; SD ; arithmetic standard deviation ; 蟽g ; geometric standard
- 刊名：Cellular Signalling
- 出版年：July 2014
- 年：2014
- 卷：26
- 期：7
- 页码：1576-1588
- 全文大小：1535 K
文摘
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Synthetic S1P1R agonists have therapeutic potential in autoimmune disorders.
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They induce transient S1P1R signaling and intracellular receptor accumulation.
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Natural S1P induces sustained S1P1R signaling which requires receptor recycling.
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This physiological receptor recycling requires S1P degradation by S1P lyase.
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Synthetic S1P1R agonists are S1P lyase resistant and thus functional antagonists.