Description
StaurosporineisanalkaloidinitiallyproducedbyStreptomycesthatinhibitsPKCandotherproteinkinases.StaurosporineisaprecursorinthesynthesisofkinaseinhibitorsK252candPKC412.Thiscompoundexhibitsanticancer,anti-parasitic,andanti-protozoanactivities.Staurosporineinducesapoptosisinhepatocarcinomacellsbydecreasinglevelsofp38MAPK,pERK,andDNAmethyltransferase3B(DNMT3B)andincreasinglevelsofpJNK.StaurosporinealsocausescelldeathinTrypanosoma.ThiscompoundalsoinhibitsmammalianRNAsplicing.
References
ZhaoC,YinP,MeiC,etal.Down-regulationofDNAmethyltransferase3Binstaurosporine-inducedapoptosisanditsmechanisminhumanhepatocarcinomacelllines.MolCellBiochem.2013Apr;376(1-2):111-9.PMID:23397112.
BrugesG,BetancourtM,MarchM,etal.Apoptotic-likeactivityofstaurosporineinaxenicculturesofTrypanosomaevansi.RevInstMedTropSaoPaulo.2012Mar-Apr;54(2):103-8.PMID:22499424.
AukemaKG,ChohanKK,PlourdeGL,etal.Smallmoleculeinhibitorsofyeastpre-mRNAsplicing.ACSChemBiol.2009Sep18;4(9):759-68.PMID:19634919.
TanramlukD,SchreyerA,PittWR,etal.Ontheoriginsofenzymeinhibitorselectivityandpromiscuity:acasestudyofproteinkinasebindingtostaurosporine.ChemBiolDrugDes.2009Jul;74(1):16-24.PMID:19519740.