亚博电子竞技

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mTOR: 诺华、辉瑞、AZ的老药和新面孔,肿瘤、糖尿病等未来
作者: 中糖院 时间: 2020-02-04 14:30:43 浏览: 91

亚博电子竞技burudongwuleipameisubadanbai(mammalian target of rapamycin,mtor)shipi3kdanbaijimeijiazuchengyuan,tongguoyubutongdanbaijiehexingchengfuhewu: mtorfuhewu1(mtorc1)hefuhewu2(mtorc2),congerduixibaoshengzhang、daixie、zishi、diaowanghemianyiyingdadengzhongyaoshengwuxuegongnengfahuidiaojiezuoyong。

mTOR的发现

mtordequedinghebiaozhengyuleipameisu(xiluomosi)defaxianmiqiexiangguan。

1964nian,yizhijianadatanxianduicongnantaipingfuhuojiedaodeturangyangbenzhongfaxianleleipameisu,tajuyouhengaodekangzhenjun、kangzhongliuhemianyiyizhizuoyong。

亚博电子竞技weishengwuxuejiageorges nogradyshoujilefuhuojiedaobutongdiqudeturangyangben,xunzhaochijiaodaominmeiyoudeposhangfengdeyuanyin。

1975nian,renmenfaxianxishuilianmeijunchanshengleyizhongkangzhenjunhuahewu,nenggouyizhibaisenianzhujun、shigaoyangxiaobaozijunhekelimaoxuanjundeshengzhang。

1982nian,leipameisudemianyiyizhihekangzhongliugongnengbeifaxian。chungdengrenfaxianleipameisuyutaijifuanxianyigoumeifkbp1a(yechengweifkbp12)xingchengfuhewuyijiedaoqikangzengzhigongneng。tongguoduileipameisukangxingdeyichuanshaixuan,jiandingletor/drrjiyin。

亚博电子竞技1994nian,zaiburudongwuxibaozhongjiandingchumtor-fkbp12fuhewu。

cihou,yuelaiyueduodeyanjiurenyuanduimtordanbaijinxingleyanjiu,bingquedingleqizaixibaoshengzhanghegongnengzhongdezhongyaozuoyong。

亚博电子竞技mtordanbaideerjijiegouruxiatusuoshi。

lengdongdianjingxia,xiayouxinhaodanbais6k1hepras40jiehediejiazairheb–mtorc1shangdefuhewujiegouruxiatusuoshi。

mTOR靶点代表药物

老药

zuichu,mtorbadianyaowuyileipameisujiqileisiwuweizhu,tongshiyizhimtorc1hemtorc2,gaileihuahewuyongyouxiangtongdemuhejiegou,tongchanggaibianrjituan,jinxingjiegouxiushi。

leipaming(leipameisu,youchengxiluomosi,r=h),shishougeshangshidemtoryizhiji,shihuiruishougouhuishisuode,yu1999nianhuofdapizhunshangshi,yongyuyufangshenyizhizhongdepaiyifanying、linbaguanpinghuajirouzengshengzheng,2007nianzaizhongguoshangshi,gaiyaoyu2014niandaodaxiaoshoufengzhi2yimeiyuan,zhihouxiaoliangruijian。guoneihuabeizhiyao、zhongmeihuadong、zhejiangyiyaodengqiyeyongyouxiluomosifangzhiyaopiwen,danshangwuqiyekaizhanyizhixingpingjia。

temsirolimustongyangshihuiruishougouhuishisuode,rwei:

亚博电子竞技yu2007nian5yuehuofdapizhunshangshi,yongyuzhiliaoshenai,weizaizhongguoshangshi,xiaoshoufangmianchengjibujia。

亚博电子竞技nuohuayiweimosi(everolimus)derwei:

zuoweidisangeshangshidemtoryizhiji,yiweimosichengjifeiran,yu2009nian3yuehuopishangshi,muqianyihuopiyongyuyufangshenyizhizhongdepaiyifanying、zhiliaoruxianai、shenjingneifenmiai、shenai、jiejiexingyinghuazhengdeng。yiweimosi2019nianxiaoshouegaoda20.2yimeiyuan,20nianxiaoliangxiahuazhi15.2yimeiyuan。muqianyizaizhongguoshangshi,wufangzhiyaoshangshi,qieweiyouqiyeqidongbeshiyan。

ciwai,zotarolimus、umirolimus、novolimusdengbeiyongyuxueguanzhijiatuceng,fahuikangpaiyizuoyong。

亚博电子竞技huirui、nuohuamuqianjunrengzaikaifatemsirolimus、yiweimosiqitazhongliushiyingzheng,bufenshiyingzhengyizhiiiiqi、iiqilinchuangjieduan;ribenzhiyaoqiyenobelpharmazejixuzairibenkaifaxiluomosiqitashiyingzheng,rudianxian、duofaxingshenjingxianweiliudeng。

新面孔

亚博电子竞技leipameisujiqileisiwuyinzuoyongyumtor,duimtorc1hemtorc2chanshengwuchabieyizhi,erchanshengjiaoduodufuzuoyong,lingyifangmianshouxinhaodiaokongyingxiangzhongliuxibaoyichanshengnaiyaoxing。

tongshiyizhishangyoupip3hexiayoumtorkejianshaozhongliuchanshengnaiyaoxing。

亚博电子竞技paxalisibfenzijiegou

亚博电子竞技muqian,pip3/mtorshuangzhongyizhijirupaxalisibyijinruiiiqilinchuang,cll-442、dactolisib、monepantel、erapa、onatasertib、bimiralisib、sf-1126yijinruiiqilinchuang。

qita,duobadiantongshiyizhimtordeyaowurujianpisuxiangguantaidiaojiejisel-403、hhyizhiacc-006dengyiyijinruiiqilinchuangjieduan。

亚博电子竞技lingyouwenxianbaodao,zhongyaojianghuangsu、fulingwan、xiangdousudengdouketongguopi3k/akt/mtortongluchanshengxiaoguo。

asilikanggengshishejilezhenduimtorbutongweidiandeyizhiji——azd-8055,yichengazd-3147,muqian,jiaozhiliushiyingzhengyijinruiqilinchuangjieduan。

jiazhoudaxuebokelifenxiaoyanjiurenyuanjiangyuazd-314tongzuoyongweidiandemln0128yuleipameisuyonglinkerlianjieqilai,xingchengraplink-1。

亚博电子竞技raplink-1zaixibaoshuipingxiazhongliuyizhixiaoguogengjia。

亚博电子竞技yeyouyixieqiyechangshixinxingfufangzhijibingqudezhongdatupo,ruracemetyrosinehuofdashouyuyixianaigueryaodiwei。


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