Description
Epothiloneisananticancerchemotherapeuticthatactsasananti-mitoticcompound;itbindsthetaxanepocketofβ-tubulin,usingsidechainstoinduceformationofashorthelixandpreventingmicrotubuledepolymerization.EpothilonedisplaysactivityagainstlungcancerandprostatecancerinclinicaltrialsandmayshowbenefitintreatmentofneurodegenerativediseasessuchasAlzheimer’sdisease.Typically,thedegreeofchemotherapeuticactivityofthethreeepothilonesubtypesfollowsthealphabet,whereEpoA>EpoB>EpoD.
References
ProtaAE,BargstenK,ZurwerraD,etal.Molecularmechanismofactionofmicrotubule-stabilizinganticanceragents.Science.2013Feb1;339(6119):587-90.PMID:23287720.
EntwistleRA,RizkRS,ChengDM,etal.Differentiatingbetweenmodelsofepothilonebindingtomicrotubulesusingtubulinmutagenesis,cytotoxicity,andmolecularmodeling.ChemMedChem.2012Sep;7(9):1580-6.PMID:22807375.
EdelmanMJ,ShvartsbeynM.Epothilonesindevelopmentfornon--small-celllungcancer:novelanti-tubulinagentswiththepotentialtoovercometaxaneresistance.ClinLungCancer.2012May;13(3):171-80.PMID:22133291
KellyWK.Epothilonesinprostatecancer.UrolOncol.2011Jul-Aug;29(4):358-65.PMID:19914096.
Rusinska-RoszakD,TatkaH,PawlakR,etal.ExtendedandclusteredconformersofepothiloneA.JPhysChemB.2011Apr7;115(13):3698-707.PMID:21405036.
LeeJJ,KellyWK.Epothilones:tubulinpolymerizationasanoveltargetforprostatecancertherapy.NatClinPractOncol.2009Feb;6(2):85-92.PMID:19048010.