G蛋白偶联受体作为药物靶点

L. Nikitha
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引用次数: 0

摘要

G-蛋白偶联受体是细胞表面受体中最大的一类,在人类基因组中有大约1000个基因编码。g蛋白偶联受体是迄今为止现代药物的最大靶标。当前围绕GPCR的同质油聚合,异质油聚合的思考,并显示了新模型如何指向新疗法开发中未探索的途径。许多疾病和失调都与gpcr的突变和多态性有关。它们是越来越多的治疗剂的目标。据估计,50%的现代药物和近四分之一的2000年最畅销的200种药物都能调节GPCR的活性。对于许多其他类型的受体,如酪氨酸激酶,配体诱导的油聚合早已被认为是信号传导的必要条件。制药行业面临的最大挑战将是将GPCR的同源和异质油聚合整合到分子模型中,用于开发新的和改进的治疗方法。将油聚化受体模型纳入GPCR药物发现策略可能会产生针对这些受体的更好的治疗药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
G protein couple receptors used as Drug target
The G- Protein coupled receptors are the largest class of cell-surface receptors and are encoded by > 1000 genes in the human genome. G-protein coupled receptors represented by far the largest class of targets for modern drugs. The current thinking surrounding GPCR homo-oilgomerization, hetero- oilgomerization and shows how new models point towards unexplored avenues in the development of new therapies. Numerous diseases and disorders have been linked mutations and Polymorphisms in GPCRs. They are the targets of an increasingly large number of therapeutic agents. It has been estimated that 50% of all modern drugs and almost one-quarter of the top 200 best – sellingdrugs in 2000 modulate GPCR activity. For many other classes of receptors such as tyrosine – kinase, ligand induced oilgomerization has long been known to be the essential for signalling. The greatest challenge facing the pharmaceutical industry will be to integrate GPCR homo- and hetero- oilgomerization into the molecular models that are used in the development of novel and improved therapeutics. The incorporation of oilgomerization receptor models into strategies for GPCR drug discovery might result in better therapeutic agents that target these receptors.
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