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首页> 外文期刊>Biotechnology Advances: An International Review Journal >An overview of the diverse roles of G-protein coupled receptors (GPCRs) in the pathophysiology of various human diseases.
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An overview of the diverse roles of G-protein coupled receptors (GPCRs) in the pathophysiology of various human diseases.

机译：G蛋白偶联受体（GPCR）在各种人类疾病的病理生理学中的不同作用概述。

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G-protein coupled receptors (GPCRs) modulate diverse cellular responses to the majority of neurotransmitters and hormones within the human body. They exhibit much structural and functional diversity, and are responsive to a plethora of endogenous (biogenic amines, cations, lipids, peptides, and glycoproteins) and exogenous (therapeutic drugs, photons, tastants, and odorants) ligands and stimuli. Due to the key roles of GPCRs in tissue/cell physiology and homeostasis, signaling pathways associated with GPCRs are implicated in the pathophysiology of various diseases, ranging from metabolic, immunological, and neurodegenerative disorders, to cancer and infectious diseases. Approximately 40% of clinically approved drugs mediate their effects by modulating GPCR signaling pathways, which makes them attractive targets for drug screening and discovery. The pace of discovery of new GPCR-based drugs has recently accelerated due to rapid advancements in high-resolution structure determination, high-throughput screening technology and in silico computational modeling of GPCR binding interaction with potential drug molecules. This review aims to provide an overview of the diverse roles of GPCRs in the pathophysiology of various diseases that are the major focus of biopharmaceutical research as potential drug targets.Digital Object Identifier http://dx.doi.org/10.1016/j.biotechadv.2013.08.017
机译：G蛋白偶联受体（GPCR）调节对人体中大多数神经递质和激素的多种细胞反应。它们具有很大的结构和功能多样性，并且对大量内源性（生物胺，阳离子，脂质，肽和糖蛋白）和外源性（治疗药物，光子，味觉和气味剂）配体和刺激物有反应。由于GPCR在组织/细胞生理和体内平衡中的关键作用，与GPCR相关的信号通路与各种疾病的病理生理有关，从代谢，免疫和神经退行性疾病到癌症和传染病。大约40％的临床批准药物通过调节GPCR信号通路来介导其作用，这使其成为有吸引力的药物筛选和发现靶标。由于高分辨率结构确定，高通量筛选技术以及GPCR与潜在药物分子相互作用的计算机模拟，近来由于基于GPCR的新药物的发现步伐加快了。这篇综述旨在概述GPCR在各种疾病的病理生理中的各种作用，这些疾病是作为潜在药物靶标的生物药物研究的主要重点。数字对象标识符http://dx.doi.org/10.1016/j.biotechadv .2013.08.017

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