钙敏感受体(CaSR )是一种在机体广泛表达的G蛋白耦联受体(GPCRs)，介导很多组织特异性功能。这种受体具有多配体的特点，而且在不同的信号通路中起不同的作用，并通过控制周围信号通路来介导其效应。

        2015年4月在《Trends in pharmacological sciences》(药理学趋势)杂志发表的一篇文章对“偏置信号”("偏向"Biasedsignaling")进行了介绍，它是由特定配体稳定优于其他受体信号引发的现象。钙敏感受体CaSR 的偏置信号由其内源性配体诱发。有趣的是，钙敏感受体CaSR的自然偏置能够改变疾病状态，且小分子药物产生的变构偏置信号能够调节下游信号转导通路。因此，钙敏感受体CaSR的偏置信号转导研究对病理生理和药物治疗效果有重要的意义。该文章对这些内容进行了概述，同时扩展到其他G蛋白耦联受体(GPCRs)。文章以钙敏感受体CaSR的配体为模型研究预偏置信号，并研究如何根据组织特异性选择不同活性的药物。

        Trends Pharmacol Sci. 2015 Apr;36(4):215-225. doi: 10.1016/j.tips.2015.02.004. Epub 2015 Mar 9.

        Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias.

        Leach K1, Conigrave AD2, Sexton PM3, Christopoulos A3.

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        Abstract

        The calcium-sensing receptor (CaSR) is a widely expressed G protein-coupled receptor (GPCR) that mediates numerous tissue-specific functions. Its multiple ligands and diverse roles attest to the need for exquisite control over the signaling pathways that mediate its effects. 'Biased signaling' is the phenomenon by which distinct ligands stabilize preferred receptor signaling states. The CaSR is subject to biased signaling in response to its endogenous ligands. Interestingly, the 'natural' bias of the CaSR is altered in disease states, and small molecule drugs engender biased allosteric modulation of downstream signaling pathways. Thus, biased signaling from the CaSR also has important implications pathophysiologically and therapeutically. As outlined in this review, this novel paradigm extends to other GPCRs, making the CaSR a model for studies of ligand-biased signaling and for understanding how it may be used to foster selective drug activity in different tissues.