Description
Neomycinisapolycationicaminoglycosideantibioticthatexhibitsantibacterialandneuromodulatoryactivities;itwasoriginallyfoundinspeciesofStreptomyces.Neomycinbindsto23SrRNA,constrainingtRNAintheP-site,inhibitingtranslocationandribosomalrecycling;together,thisresultsininhibitionofproteinsynthesis.NeomycinBbindsandinhibitsbacterialRNasePandbacterialTboxantiterminatorRNA.NeomycinBinhibitsmammalianRNAsplicingaswell.Neomycinalsononcompetitivelyinhibitscationchannels,includingP2Xreceptorsandtransientreceptorpotentialvanilloidreceptor1(TRPV1)channels.Additionally,thiscompoundinhibitsCa2+influx,preventingpresynapticreleaseofacetylcholineandnorepinephrineinfelinesuperiorcervicalganglia.
References
WangL,PulkA,WassermanMR,etal.Allostericcontroloftheribosomebysmall-moleculeantibiotics.NatStructMolBiol.2012Sep;19(9):957-63.PMID:22902368.
BongartzEV,RettingerJ,HausmannR.AminoglycosideblockofP2X2receptorsheterologouslyexpressedinXenopuslaevisoocytes.PurinergicSignal.2010Dec;6(4):393-403.PMID:21437010.
AukemaKG,ChohanKK,PlourdeGL,etal.Smallmoleculeinhibitorsofyeastpre-mRNAsplicing.ACSChemBiol.2009Sep18;4(9):759-68.PMID:19634919.
AnupamR,DenapoliL,MuchenditsiA,etal.IdentificationofneomycinB-bindingsiteinTboxantiterminatormodelRNA.BioorgMedChem.2008Apr15;16(8):4466-70.PMID:18329274.
KawamotoSA,SudhaharCG,HatfieldCL,etal.StudiesonthemechanismofinhibitionofbacterialribonucleasePbyaminoglycosidederivatives.NucleicAcidsRes.2008Feb;36(2):697-704.PMID:18084035.
RaisinghaniM,PremkumarLS.Blockofnativeandclonedvanilloidreceptor1(TRPV1)byaminoglycosideantibiotics.Pain.2005Jan;113(1-2):123-33.PMID:15621372.
WrightJM,CollierB.Theeffectsofneomycinupontransmitterreleaseandaction.JPharmacolExpTher.1977Mar;200(3):576-87.PMID:191590.