典型文献
Structural insights into sphingosine-1-phosphate recognition and ligand selectivity of S1PR3-Gi signaling complexes
文献摘要：
Dear Editor,
Lipids are essential for all life on earth and play critical roles in energy storage and the formation of cellular membranes.Sphingosine-1-phosphate (S1P) is a naturally occurring bioactive lysophospholipid that regulates fundamental physiological processes by activating five G protein-coupled receptors (S1PR1-S1 PR5).S1 PRs are widely distributed on many cell types,including cells in the cardiovascular,immune,and central nervous systems.1 The multi-functional S1P-S1PR signaling is a driver of multiple diseases and S1PR1-targeted drugs have been approved as therapeutic strategies for the treatment of multiple sclerosis (MS) and autoimmune disorders.The first approved drug fingolimod (FTY720),after in-vivo phosphorylation to pFTY720,has cross reactivity with the S1PR family(S1PR1-3 and S1PR5),and subtype-selective modulators have been pursued as potential therapeutics.Siponimod is selective for S1PR1 and S1PR5 and has been approved for the treatment of secondary progressive MS.Molecules that lack S1PR3-targeting activity may be a useful strategy for the development of S1PR1 agonist drugs.2 Therefore,understanding the mechanism of S1P-S1PR signaling and identifying differences in the ligand selectivity of the S1 PR family may assist in the development of drugs with improved safety profiles for the control of MS,cardiovascular and autoimmune disorders.
文献关键词：
中图分类号：
作者姓名：
Chang Zhao;Lin Cheng;Wei Wang;Heli Wang;Yongbo Luo;Yuying Feng;Xuehui Wang;Hong Fu;Ye Cai;Shengyong Yang;Ping Fu;Wei Yan;Zhenhua Shao
作者机构：
Division of Nephrology and Kidney Research Institute,State Key Laboratory of Biotherapy and Cancer Center,West China Hospital,Sichuan University,Chengdu,Sichuan,China
文献出处：
引用格式：
[1]Chang Zhao;Lin Cheng;Wei Wang;Heli Wang;Yongbo Luo;Yuying Feng;Xuehui Wang;Hong Fu;Ye Cai;Shengyong Yang;Ping Fu;Wei Yan;Zhenhua Shao-.Structural insights into sphingosine-1-phosphate recognition and ligand selectivity of S1PR3-Gi signaling complexes)[J].细胞研究（英文版）,2022(02):218-221
A类：
Lipids,lysophospholipid,S1PR,fingolimod,FTY720,pFTY720,S1PR5,Siponimod
B类：
Structural,insights,into,sphingosine,phosphate,recognition,ligand,selectivity,S1PR3,Gi,signaling,complexes,Dear,Editor,are,essential,life,earth,play,critical,roles,energy,storage,formation,cellular,membranes,Sphingosine,naturally,occurring,bioactive,that,regulates,fundamental,physiological,processes,by,activating,five,protein,coupled,receptors,S1PR1,PRs,widely,distributed,many,types,including,cells,cardiovascular,central,nervous,systems,functional,driver,multiple,diseases,targeted,drugs,have,been,approved,strategies,treatment,sclerosis,autoimmune,disorders,first,after,vivo,phosphorylation,has,cross,reactivity,family,subtype,selective,modulators,pursued,potential,therapeutics,secondary,progressive,Molecules,lack,targeting,may,useful,strategy,development,agonist,Therefore,understanding,mechanism,identifying,differences,assist,improved,safety,profiles,control
AB值：
0.517172
相似文献
机标中图分类号，由域田数据科技根据网络公开资料自动分析生成，仅供学习研究参考。
