Differential Modulation of Beta-Adrenergic Receptor Signaling by Trace Amine-Associated Receptor 1 Agonists 英文参考文献.docVIP

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Differential Modulation of Beta-Adrenergic Receptor Signaling by Trace Amine-Associated Receptor 1 Agonists 英文参考文献.doc

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Differential Modulation of Beta-Adrenergic Receptor Signaling by Trace Amine-Associated Receptor 1 Agonists 英文参考文献

DifferentialModulationofBeta-AdrenergicReceptor SignalingbyTraceAmine-AssociatedReceptor1 Agonists GunnarKleinau1.,JulianePratzka1.,DanielaNu¨rnberg1,AnnetteGru¨ters1,DagmarFu¨hrer-Sakel3, HeikoKrude1,JosefKo¨hrle2,TorstenScho¨neberg4,HeikeBiebermann1* 1Institute of Experimental Pediatric Endocrinology, Berlin, Berlin, Germany, 2Institute of Experimental Endocrinology, Charite′-Universita¨tsmedizin Charite′- Universita¨tsmedizin Berlin, Berlin, Germany, 3Klinik fu¨r Endokrinologie, Zentrum fu¨r Innere Medizin, Universita¨tsklinikum Essen, Essen, Germany, 4Institute of Biochemistry,MedicalFaculty,UniversityofLeipzig,Leipzig,Germany Abstract Trace amine-associated receptors (TAAR) are rhodopsin-like G-protein-coupled receptors (GPCR). TAAR are involved in modulation of neuronal, cardiac and vascular functions and they are potentially linked with neurological disorders like schizophreniaandParkinson’sdisease.SubtypeTAAR1,thebestcharacterizedTAARsofar,ispromiscuousforawidesetof ligands and is activated by trace amines tyramine (TYR), phenylethylamine (PEA), octopamine (OA), but also by thyronamines, dopamine, and psycho-active drugs. Unfortunately, effects of trace amines on signaling of the two homologousb-adrenergicreceptors1(ADRB1)and2(ADRB2)havenotbeenclarifiedyetindetail.We,therefore,tested TAAR1agonistsTYR,PEAandOAregardingtheireffectsonADRB1/2signalingbyco-stimulationstudies.Surprisingly,trace aminesTYRandPEAarepartialallostericantagonistsatADRB1/2,whereasOAisapartialorthostericADRB2-antagonistand ADRB1-agonist.TospecifymolecularreasonsforTAAR1ligandpromiscuityandforobserveddifferencesinsignalingeffects onparticularaminergicreceptorswecomparedTAAR,tyramine(TAR)octopamine(OAR),ADRB1/2anddopaminereceptors atthestructurallevel.WefoundespeciallyforTAAR1thattheremarkableligandpromiscuityislikelybasedonhighamino acidsimilarityintheligand-bindingregioncomparedwithfurtheraminergicreceptors.Onth