Description
MK-1775isaninhibitorofWee1,aproteinthatregulatestheG2mitosischeckpointinresponsetoDNAdamage.MK-1775exhibitsanticancerchemotherapeuticactivity.Inacutemyelogenousleukemia(AML)cells,thiscompounddecreasesphosphorylationofCDK1/2andinducesdouble-strandedDNAbreaks.Inanimalmodelsofvariouscancers,MK-1775increasessurvivaltimesanddecreasestumorsize,particularlywhenco-admiNISTeredwithothertreatments.
References
QiW,XieC,LiC,etal.CHK1playsacriticalroleintheanti-leukemicactivityofthewee1inhibitorMK-1775inacutemyeloidleukemiacells.JHematolOncol.2014Aug1;7:53.PMID:25084614.
VanLindenAA,BaturinD,FordJB,etal.InhibitionofWee1sensitizescancercellstoantimetabolitechemotherapeuticsinvitroandinvivo,independentofp53functionality.MolCancerTher.2013Dec;12(12):2675-84.PMID:24121103.
HiraiH,IwasawaY,OkadaM,etal.Small-moleculeinhibitionofWee1kinasebyMK-1775selectivelysensitizesp53-deficienttumorcellstoDNA-damagingagents.MolCancerTher.2009Nov;8(11):2992-3000.PMID:19887545.