Discovery of Novel Proteasome Inhibitors Using a High-Content Cell-Based Screening System 英文参考文献.docVIP

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Discovery of Novel Proteasome Inhibitors Using a High-Content Cell-Based Screening System 英文参考文献.doc

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Discovery of Novel Proteasome Inhibitors Using a High-Content Cell-Based Screening System 英文参考文献

DiscoveryofNovelProteasomeInhibitorsUsingaHigh- ContentCell-BasedScreeningSystem IrenaLavelin1,AvitalBeer2,ZviKam1,VardaRotter1,MosheOren1,AmiNavon2,BenjaminGeiger1* 1DepartmentofMolecularCellBiology,WeizmannInstituteofScience,Rehovot,Israel,2DepartmentofBiologicalRegulation,WeizmannInstituteofScience,Rehovot, Israel Abstract Theregulateddegradationofdamagedormisfoldedproteins,aswellasdown-regulationofkeysignalingproteins,within eukaryotic and bacterial cells is catalyzed primarily by large, ATP-dependent multimeric proteolytic complexes, termed proteasomes.Inhibitionofproteasomalactivityaffectsawidevarietyofphysiologicalandpathologicalprocesses,andwas foundtobeparticularlyeffectiveforcancertherapy.Wereporthereonthedevelopmentofanovelhighthroughputassay for proteasome inhibition using a unique, highly sensitive live-cell screening, based on the cytoplasm-to-nucleus translocationofafluorescentproteasomeinhibitionreporter(PIR)protein,consistingofnuclearlocalizationsignal-deficient p53derivative.Wefurthershowherethatmdm2,akeynegativeregulatorofp53playsakeyroleintheaccumulationofPIR in the nucleus upon proteasome inhibition. Using this assay, we have screened the NCI Diversity Set library, containing 1,992 low molecularweight synthetic compounds, andidentified four proteasome inhibitors.The specialfeatures of the currentscreen,comparedtothoseofotherapproachesarediscussed. Citation: Lavelin I, Beer A, Kam Z, Rotter V, Oren M, et al. (2009) Discovery of Novel Proteasome Inhibitors Using a High-Content Cell-Based Screening System.PLoSONE4(12):e8503.doi:10.1371/journal.pone.0008503 Editor:AnilKumarTyagi,UniversityofDelhi,India ReceivedSeptember8,2009;AcceptedDecember8,2009;PublishedDecember30,2009 Copyright: ? 2009 Lavelin et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricteduse,distribution,andreproductioninanymedium,providedtheoriginalauthorandsourcearecredited. Funding:Thisstudywassupport