典型文献
GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation in macrophages
文献摘要：
The putative medium-chain free fatty acid receptor GPR84 is a G protein-coupled receptor primarily expressed in myeloid cells that constitute the innate immune system,including neutrophils,monocytes,and macrophages in the periphery and microglia in the brain.The fact that GPR84 expression in leukocytes is remarkably increased under acute inflammatory stimuli such as lipopolysaccharide(LPS)and TNFα suggests that it may play a role in the development of inflammatory and fibrotic diseases.Here we demonstrate that GPR84 is highly upregulated in inflamed colon tissues of active ulcerative colitis(UC)patients and dextran sulfate sodium(DSS)-induced colitis mice.Infiltrating GPR84+macrophages are significantly increased in the colonic mucosa of both the UC patients and the mice with colitis.Consistently,GPR84-/-mice are resistant to the development of colitis induced by DSS.GPR84 activation imposes pro-inflammatory properties in colonic macrophages through enhancing NLRP3 inflammasome activation,while the loss of GPR84 prevents the M1 polarization and properties of proinflammatory macrophages.CLH536,a novel GPR84 antagonist discovered by us,suppresses colitis by reducing the polarization and function of pro-inflammatory macrophages.These results define a unique role of GPR84 in innate immune cells and intestinal inflammation,and suggest that GPR84 may serve as a potential drug target for the treatment of UC.
文献关键词：
中图分类号：
作者姓名：
Qing Zhang;Lin-hai Chen;Hui Yang;You-chen Fang;Si-wei Wang;Min Wang;Qian-ting Yuan;Wei Wu;Yang-ming Zhang;Zhan-ju Liu;Fa-jun Nan;Xin Xie
作者机构：
State Key Laboratory of Drug Research,The National Center for Drug Screening,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China;School of Pharmaceutical Science and Technology,Hangzhou Institute for Advanced Study,University of Chinese Academy of Sciences,Hangzhou 310024,China;University of Chinese Academy of Sciences,Beijing 100049,China;Department of Gastroenterology,The Shanghai Tenth People's Hospital,Tongji University,Shanghai 200072,China;Burgeon Therapeutics Co.,Ltd,Shanghai 201203,China;Yantai Key Laboratory of Nanomedicine and Advanced Preparations,Yantai Institute of Materia Medica,Yantai 264000,China
文献出处：
引用格式：
[1]Qing Zhang;Lin-hai Chen;Hui Yang;You-chen Fang;Si-wei Wang;Min Wang;Qian-ting Yuan;Wei Wu;Yang-ming Zhang;Zhan-ju Liu;Fa-jun Nan;Xin Xie-.GPR84 signaling promotes intestinal mucosal inflammation via enhancing NLRP3 inflammasome activation in macrophages)[J].中国药理学报（英文版）,2022(08):2042-2054
A类：
GPR84,Infiltrating,GPR84+macrophages,CLH536
B类：
signaling,promotes,intestinal,mucosal,inflammation,via,enhancing,NLRP3,inflammasome,activation,putative,medium,chain,free,fatty,acid,receptor,protein,coupled,primarily,expressed,myeloid,cells,that,constitute,innate,immune,system,including,neutrophils,monocytes,periphery,microglia,brain,fact,expression,leukocytes,remarkably,increased,under,acute,stimuli,such,lipopolysaccharide,LPS,suggests,may,play,role,development,fibrotic,diseases,Here,we,demonstrate,highly,upregulated,inflamed,tissues,active,ulcerative,colitis,UC,patients,dextran,sulfate,sodium,DSS,induced,mice,are,significantly,colonic,both,Consistently,resistant,by,imposes,properties,through,while,loss,prevents,M1,polarization,proinflammatory,novel,antagonist,discovered,us,suppresses,reducing,function,These,results,define,unique,serve,potential,drug,target,treatment
AB值：
0.50516
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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。
