Insights into the regulation of 5-HT2A serotonin receptors by scaffolding proteins and kinases.

Insights into the regulation of 5-HT2A serotonin receptors by scaffolding proteins and kinases.
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DOI:
10.1016/j.neuropharm.2008.06.048
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发表时间:
2008-11
期刊:
影响因子:
4.7
通讯作者:
Roth, Bryan L.
Roth, Bryan L.
中科院分区:
医学2区
文献类型:
--
作者:
Allen, John A.;Yadav, Prern N.;Roth, Bryan L.

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5-HT 2A血清素受体是LSD样致幻剂和非典型抗精神病药物作用的重要分子靶点。5-HT 2A血清素受体还介导外周和中枢神经系统中的多种生理过程,包括血小板聚集、平滑肌收缩以及情绪和感知的调节。支架蛋白已成为5-HT 2A受体的重要调节因子,我们最近的研究表明5-HT 2A受体存在多种支架,包括PSD 95,arrestin和caveolin。此外,p90核糖体S6激酶和5-HT 2A受体之间出现了一种新的相互作用,这种相互作用减弱了受体信号传导。本文综述了我们最近的研究,并强调了支架蛋白和激酶在5-HT 2A运输,靶向和信号转导的调节中的作用。
5-HT2A serotonin receptors are essential molecular targets for the actions of LSD-like hallucinogens and atypical antipsychotic drugs. 5-HT2A serotonin receptors also mediate a variety of physiological processes in peripheral and central nervous systems including platelet aggregation, smooth muscle contraction, and the modulation of mood and perception. Scaffolding proteins have emerged as important regulators of 5-HT2A receptors and our recent studies suggest multiple scaffolds exist for 5-HT2A receptors including PSD95, arrestin, and caveolin. In addition, a novel interaction has emerged between p90 ribosomal S6 kinase and 5-HT2A receptors which attenuates receptor signaling. This article reviews our recent studies and emphasizes the role of scaffolding proteins and kinases in the regulation of 5-HT2A trafficking, targeting and signaling.
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