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Dimers of serotonin receptors: Impact on ligand affinity and signaling
Biochimie ( IF 3.3 ) Pub Date : 2019-01-24 , DOI: 10.1016/j.biochi.2019.01.009
Luc Maroteaux , Catherine Béchade , Anne Roumier

Membrane receptors often form complexes with other membrane proteins that directly interact with different effectors of the signal transduction machinery. G-protein-coupled receptors (GPCRs) were for long time considered as single pharmacological entities. However, evidence for oligomerization appeared for various classes and subtypes of GPCRs. This review focuses on metabotropic serotonin (5-hydroxytryptamine, 5-HT) receptors, which belong to the rhodopsin-like class A of GPCRs, and will summarize the convergent evidence that homo- and hetero-dimers containing 5-HT receptors exist in transfected cells and in-vivo. We will show that complexes involving 5-HT receptors may acquire new signal transduction pathways and new physiological roles. In some cases, these complexes participate in disease-specific deregulations, that can be differentially affected by various drugs. Hence, selecting receptor complex-specific responses of these heterodimers may constitute an emerging strategy likely to improve beneficial therapeutic effects.



中文翻译:

血清素受体的二聚体:对配体亲和力和信号传导的影响

膜受体通常与其他膜蛋白形成复合物,这些膜蛋白直接与信号转导机制的不同效应子相互作用。长期以来,G蛋白偶联受体(GPCR)被视为单一药理实体。但是,对于GPCR的各种类型和亚型,均出现了低聚的证据。这篇综述着重于代谢型5-羟色胺(5-羟色胺,5-HT)受体,该受体属于类视紫红质的GPCR,并总结了汇聚的证据表明转染的中存在含5-HT受体的同型和异型二聚体。细胞和体内。我们将显示涉及5-HT受体的复合物可能获得新的信号转导途径和新的生理作用。在某些情况下,这些复合物会参与特定于疾病的放松,这可能会受到各种药物的不同影响。因此,选择这些异二聚体的受体复合物特异性应答可能构成可能改善有益治疗效果的新兴策略。

更新日期:2019-01-24
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