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1-磷酸鞘氨醇受体配体的选择性和特异性:“脱靶效应”还是复杂药理学?

Selectivity and specificity of sphingosine 1-phosphate receptor ligands: "off-targets" or complex pharmacology?

作者信息

Pyne Nigel J, Pyne Susan

机构信息

Cell Biology Group, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde Glasgow, UK.

出版信息

Front Pharmacol. 2011 May 31;2:26. doi: 10.3389/fphar.2011.00026. eCollection 2011.

DOI:10.3389/fphar.2011.00026
PMID:21687518
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3108476/
Abstract

A recent perspective published in Frontiers of Pharmacology by Salomone and Waeber (2011) discussed the selectivity and specificity of sphingosine 1-phosphate (S1P) receptor ligands. This perspective surveyed the use of various S1P receptor ligands and attempted to reconcile a number of inconsistencies in the predicted biological outcomes: these were interpreted as "off-target" effects. Therefore the perspective cautioned against the use of these S1P receptor ligands. Here we highlight the complex pharmacology of S1P receptors, which along with "inside-out" signaling might provide an alternative explanation for "off-target" effects.

摘要

萨洛莫内和韦贝尔(2011年)近期发表于《药理学前沿》的一篇观点文章讨论了1-磷酸鞘氨醇(S1P)受体配体的选择性和特异性。该观点文章综述了各种S1P受体配体的应用,并试图调和预测生物学结果中存在的一些不一致之处:这些不一致被解释为“脱靶”效应。因此,该观点文章告诫不要使用这些S1P受体配体。在此,我们强调S1P受体复杂的药理学特性,其与“由内向外”信号传导一起可能为“脱靶”效应提供另一种解释。

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