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作 者:赵强[1] 吴镭[2] 李佳[1] 吴蓓丽[1] 谢欣[1] 姜威[2] 孟庆峰[2] 董尔丹[2]
机构地区:[1]中国科学院上海药物研究所,上海201203 [2]国家自然科学基金委员会,北京100085
出 处:《中国基础科学》2015年第3期3-8,25,共7页China Basic Science
摘 要:G蛋白偶联受体(GPCR)超家族是数目最多并具有重要生理功能的一类受体,其功能紊乱与许多重大疾病的发生、发展密切相关。据统计,世界上约45%的临床药物直接靶向GPCR及其信号转导途径。当今,全球新药研发进入低谷,针对靶点的药物研发遇到瓶颈,如何有机整合GPCR领域的最新进展,有效衔接以GPCR为药靶的基础研究、临床研究和药物研发是该领域继续引领全球生物医药发展的关键。鉴于GPCR在重大疾病研究中的作用及发展前景,重大疾病导向的G蛋白偶联受体结构、功能和配体发现研究十分迫切。G-protein coupled receptor( GPCR) superfamily is the largest protein family within human genome and has various physiological roles. Dysfunction of these receptors often leads to significant human diseases. Up to date,there are about 45% of marketed drugs are directly targeting on GPCRs or their pathways. The global drug discovery is currently hitting a bottleneck,and integrating the basic research,clinical research and drug development targeting on GPCRs becomes more and more important. In the light of their roles and perspectives in the treatment of important human diseases,the structural and functional research,as well as ligand development based on GPCRs related to important human diseases is extremely urgent.
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