典型文献
FXR:structures,biology,and drug development for NASH and fibrosis diseases
文献摘要：
The nuclear receptor farnesoid-X-receptor(FXR)plays an essential role in bile acid,glucose,and lipid homeostasis.In the last two decades,several diseases,such as obesity,type 2 diabetes,nonalcoholic fatty liver disease,cholestasis,and chronic inflammatory diseases of the liver and intestine,have been revealed to be associated with alterations in FXR functions.FXR has become a promising therapeutic drug target,particularly for enterohepatic diseases.Despite the large number of FXR modulators reported,only obeticholic acid(OCA)has been approved for primary biliary cholangitis(PBC)therapy as FXR modulator.In this review,we summarize the structure and function of FXR,the development of FXR modulators,and the structure-activity relationships of FXR modulators.Based on the structural analysis,we discuss potential strategies for developing future therapeutic FXR modulators to overcome current limitations,providing new perspectives for enterohepatic and metabolic diseases treatment.
文献关键词：
中图分类号：
作者姓名：
Si-yu Tian;Shu-ming Chen;Cheng-xi Pan;Yong Li
作者机构：
The State Key Laboratory of Cellular Stress Biology,Innovation Center for Cell Signaling Network,School of Life Sciences,Xiamen University,Xiamen 361005,China
文献出处：
引用格式：
[1]Si-yu Tian;Shu-ming Chen;Cheng-xi Pan;Yong Li-.FXR:structures,biology,and drug development for NASH and fibrosis diseases)[J].中国药理学报（英文版）,2022(05):1120-1132
A类：
obeticholic
B类：
FXR,structures,biology,drug,development,NASH,fibrosis,diseases,nuclear,receptor,farnesoid,plays,essential,role,bile,acid,glucose,lipid,homeostasis,In,last,two,decades,several,such,obesity,type,diabetes,nonalcoholic,fatty,liver,cholestasis,chronic,inflammatory,intestine,have,been,revealed,associated,alterations,functions,has,become,promising,therapeutic,target,particularly,enterohepatic,Despite,large,number,modulators,reported,only,OCA,approved,primary,biliary,cholangitis,PBC,therapy,this,review,we,summarize,activity,relationships,Based,structural,analysis,discuss,potential,strategies,developing,future,overcome,current,limitations,providing,new,perspectives,metabolic,treatment
AB值：
0.599337
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