Conducting the G-protein Coupled Receptor (GPCR) Signaling Symphony in Cardiovascular Diseases: New Therapeutic Approaches.

Conducting the G-protein Coupled Receptor (GPCR) Signaling Symphony in Cardiovascular Diseases: New Therapeutic Approaches.
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DOI:
10.1016/j.ddmod.2012.03.001
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发表时间:
2012
期刊:
Drug discovery today. Disease models
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G蛋白偶联受体(GPCR)是一类几乎无处不在的膜结合受体,其功能性地将激素或神经递质信号与生理反应偶联。GPCR信号转导的失调有助于许多心血管疾病的病理生理学。几十年来,靶向GPCR的药理学试剂已被确立为治疗选择。然而,心血管疾病的持续负担需要改进治疗。为此,令人兴奋的药物开发工作已经开始集中在新的化合物,有区别地激活特定的GPCR信号通路。
G protein-coupled receptors (GPCRs) are a virtually ubiquitous class of membrane-bound receptors, which functionally couple hormone or neurotransmitter signals to physiological responses. Dysregulation of GPCR signaling contributes to the pathophysiology of a host of cardiovascular disorders. Pharmacological agents targeting GPCRs have been established as therapeutic options for decades. Nevertheless, the persistent burden of cardiovascular diseases necessitates improved treatments. To that end, exciting drug development efforts have begun to focus on novel compounds that discriminately activate particular GPCR signaling pathways.