| Journal of Leukocyte Biology: An Official Publication of the Reticuloendothelial Society | |
| Biased agonism at chemokine receptors: obstacles or opportunities for drug discovery? | |
| 关键词: GPCRs; allosteric modulators; inflammation; | |
| DOI : 10.1189/jlb.2MR0815-392R | |
| 学科分类：生理学 | |
| 来源: Federation of American Societies for Experimental Biology | |
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【 摘 要 】
Chemokinereceptorsaretypicallypromiscuous,bindingmorethanoneligand,withtheligandsthemselvesoftenexpressedindifferentspatiallocalizationsbymultiplecelltypes.Thisisnormallyatightlyregulatedprocess;however,inavarietyofinflammatorydisorders,dysregulationresultsintheexcessiveorinappropriateexpressionofchemokinesthatdrivesdiseaseprogression.Biasedagonism,thephenomenonwherebydifferentligandsofthesamereceptorareabletopreferentiallyactivateonesignalingpathwayoveranother,addsanotherlevelofcomplexitytoanalreadycomplexsystem.Inthisminireview,wediscusstheconceptofbiasedagonismwithinthechemokinefamilyandreportthattargetingsinglesignalingaxesdownstreamofchemokinereceptorsisnotonlyachievable,butmaywellpresentnovelopportunitiestotargetchemokinereceptors,allowingthefinetuningofreceptorresponsesinthecontextofallergicinflammationandbeyond...
【 授权许可】
CC BY
【 预 览 】
| Files | Size | Format | View |
|---|---|---|---|
| RO201904047398475ZK.pdf | 692KB |  download |
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