中国基础科学
中國基礎科學
중국기출과학
CHINA BASIC SCIENCE
2015年
3期
3-8,25
,共7页
赵强%吴镭%李佳%吴蓓丽%谢欣%姜威%孟庆峰%董尔丹
趙彊%吳鐳%李佳%吳蓓麗%謝訢%薑威%孟慶峰%董爾丹
조강%오뢰%리가%오배려%사흔%강위%맹경봉%동이단
G蛋白偶联受体%基础研究%药物研发
G蛋白偶聯受體%基礎研究%藥物研髮
G단백우련수체%기출연구%약물연발
G-protein coupled receptor ( GPCR)%basic research%drug development
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蛋白偶聯受體( GPCR )超傢族是數目最多併具有重要生理功能的一類受體,其功能紊亂與許多重大疾病的髮生、髮展密切相關。據統計,世界上約45%的臨床藥物直接靶嚮GPCR及其信號轉導途徑。噹今,全毬新藥研髮進入低穀,針對靶點的藥物研髮遇到瓶頸,如何有機整閤GPCR領域的最新進展,有效銜接以GPCR為藥靶的基礎研究、臨床研究和藥物研髮是該領域繼續引領全毬生物醫藥髮展的關鍵。鑒于GPCR在重大疾病研究中的作用及髮展前景,重大疾病導嚮的G蛋白偶聯受體結構、功能和配體髮現研究十分迫切。
G단백우련수체( GPCR )초가족시수목최다병구유중요생리공능적일류수체,기공능문란여허다중대질병적발생、발전밀절상관。거통계,세계상약45%적림상약물직접파향GPCR급기신호전도도경。당금,전구신약연발진입저곡,침대파점적약물연발우도병경,여하유궤정합GPCR영역적최신진전,유효함접이GPCR위약파적기출연구、림상연구화약물연발시해영역계속인령전구생물의약발전적관건。감우GPCR재중대질병연구중적작용급발전전경,중대질병도향적G단백우련수체결구、공능화배체발현연구십분박절。
G-protein coupled receptor ( GPCR) superfamily is the largest protein family within human genome and has various physiological roles.Dysfunction of these recep-tors often leads to significant human diseases.Up to date , there are about 45%of marketed drugs are direct-ly targeting on GPCRs or their pathways.The global drug discovery is currently hitting a bottleneck, and in-tegrating the basic research, clinical research and drug development targeting on GPCRs becomes more and more important.In the light of their roles and perspec-tives in the treatment of important human diseases, the structural and functional research, as well as ligand de-velopment based on GPCRs related to important human diseases is extremely urgent.