Description
SpinorphinisaheptapeptidewiththesequenceL-V-V-Y-P-W-T.Spinorphinisanendogenousenkephalinaseinhibitor,antagonizingenzymessuchasaminopeptidaseIV,neutralendopeptidase,dipeptidylpeptidaseIII(DPP3),andangiotensin-convertingenzyme(ACE);italsoactsasanantagoNISTattheP2X3receptor.Spinorphinexhibitsantinociceptive,antidepressant,gastrointestinalmotilitymodulating,anti-inflammatory,andimmunomodulatoryactivities.SpinorphinalsoactsasanantagonistatN-formylpeptidereceptors,preventingbindingofchemotacticf-MLFtoitsreceptoronpolymorphonuclear(PMN)neutrophilsandinhibitingneutrophilfunctionality.
References
ThanawalaV,KadamVJ,GhoshR.Enkephalinaseinhibitors:potentialagentsforthemanagementofpain.CurrDrugTargets.2008Oct;9(10):887-94.PMID:18855623.
JungKY,MoonHD,LeeGE,etal.Structure-activityrelationshipstudiesofspinorphinasapotentandselectivehumanP2X(3)receptorantagonist.JMedChem.2007Sep6;50(18):4543-7.PMID:17676725.
YamamotoY,OnoH,UedaA,etal.Spinorphinasanendogenousinhibitorofenkephalin-degrADIngenzymes:rolesinpainandinflammation.CurrProteinPeptSci.2002Dec;3(6):587-99.PMID:12470213.
LiangTS,GaoJL,FatemiO,etal.TheendogenousopioidspinorphinblocksfMet-Leu-Phe-inducedneutrophilchemotaxisbyactingasaspecificantagonistattheN-formylpeptidereceptorsubtypeFPR.JImmunol.2001Dec1;167(11):6609-14.PMID:11714831.
NishimuraK,HazatoT.Isolationandidentificationofanendogenousinhibitorofenkephalin-degradingenzymesfrombovinespinalcord.BiochemBiophysResCommun.1993Jul30;194(2):713-9.PMID:8343155.