Selective and Irreversible Inhibitors of Aphid Acetylcholinesterases Steps Toward Human-Safe Insecticides 英文参考文献.docVIP

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Selective and Irreversible Inhibitors of Aphid Acetylcholinesterases Steps Toward Human-Safe Insecticides 英文参考文献.doc

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Selective and Irreversible Inhibitors of Aphid Acetylcholinesterases Steps Toward Human-Safe Insecticides 英文参考文献

SelectiveandIrreversibleInhibitorsofAphid Acetylcholinesterases:StepsTowardHuman-Safe Insecticides Yuan-PingPang1*,SanjayK.Singh1¤a,YangGao1,T.LeonLassiter1¤b,RajeshK.Mishra1,KunYanZhu2, StephenBrimijoin1* 1Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Rochester, Minnesota, United States of America, 2Department of Entomology, Kansas State University,Manhattan,Kansas,UnitedStatesofAmerica Abstract Aphids,amongthemostdestructiveinsectstoworldagriculture,aremainlycontrolledbyorganophosphateinsecticidesthat disablethecatalyticserineresidueofacetylcholinesterase(AChE).BecausetheseagentsalsoaffectvertebrateAChEs,theyare toxictonon-targetspeciesincludinghumansandbirds.Wepreviouslyreportedthatacysteineresidue(Cys),foundatthe AChEactivesiteinaphidsandotherinsectsbutnotmammals,mightserveasatargetforinsect-selectivepesticides.However, aphidshavetwodifferentAChEs(termedAPandAO),andonlyAP-AChEcarriestheuniqueCys.Theabsenceoftheactive-site Cys in AO-AChEmight raise concerns about the utility of targeting thatresidue. Herein we reportthe development of a methanethiosulfonate-containingsmallmoleculethat,at6.0mM,irreversiblyinhibits99%ofallAChEactivityextractedfrom thegreenbugaphid(Schizaphisgraminum)withoutanymeasurableinhibitionofthehumanAChE.Reactivationstudiesusing b-mercaptoethanolconfirmthattheirreversibleinhibitionresultedfromtheconjugationoftheinhibitortotheuniqueCys. TheseresultssuggestthatAO-AChEdoesnotcontributesignificantlytotheoverallAChEactivityinaphids,thusofferingnew insightintotherelativefunctionalimportanceofthetwoinsectAChEs.Moreimportantly,bydemonstratingthattheCys- targetinginhibitorcanabolishAChEactivityinaphids,wecanconcludethattheuniqueCysmaybeaviabletargetforspecies- selectiveagentstocontrolaphidswithoutcausinghumantoxicityandresistanceproblems. Citation:PangY-P,SinghSK,GaoY,LassiterTL,MishraRK,etal.(2009)SelectiveandIrreversibleInhibitorsofAphidAcetylcholinesterases:StepsTowardHuman- SafeInsecticides.PLoSONE4(2):e4349.doi:10.1371/jour