Signaltransducerandactivatoroftranscription3(STAT3)regulatesmanycriticalfunctionsinhumannormalandmalignanttissues,suchasdifferentiation,proliferation,survival,angiogenesisandimmunefunction.ConstitutiveactivationofSTAT3isimplicatedinawiderangeofhumancancers.Assuch,STAT3hasbeenstudiedasatumortherapeutictarget.ThelastapproachusingsmallmoleculeSTAT3inhibitorshasbeenthemostexaminedsoHeterocylesandCarbazole.Heterocylesareanessentialclassofmolecules,assumingaroleinmanyaspectofourlife.Indeedheterocyclicnucleusisacommonfeatureofseveralbiomoleculeandbioactivecompoundsincludingagrochemicalproductsanddrugs.Inthisreviewwefocusedontwoimportantclassofheterocycliccompounds:carbazolesandNHCs(N-heterocycliccarbenes)andthereimplicationsincancerinhibitions.Carbazoles,prevalentasstructuralmotifsinvarioussyntheticmaterialsandnaturallyoccurringalkaloids,asisknown,havemanyapplicationsespeciallyaspromisingbioactivecompoundsduetotheirbiologicalproperties,knownsince1965.FurthermoreNHCsareaclassofstablecarbenesthatoverthelastfewyearshaveenteredthefieldas“new”ligandsforbioactivecoordinationcompounds.IthasbeendemonstratedthatmetalNHCcomplexescanbeusedtodevelophighlyefficientmetalbaseddrugswithpossibleapplicationsinthetreatmentofcancerorinfectiousdiseases.
TARGETING STAT3 IN CANCER INHIBITION
RODRIQUEZ, Manuela;LONGO, Pasquale;MARICONDA, ANNALUISA;DE MARTINO, Franco;CAPASSO, Anna;SATURNINO, Carmela
2015
Abstract
Signaltransducerandactivatoroftranscription3(STAT3)regulatesmanycriticalfunctionsinhumannormalandmalignanttissues,suchasdifferentiation,proliferation,survival,angiogenesisandimmunefunction.ConstitutiveactivationofSTAT3isimplicatedinawiderangeofhumancancers.Assuch,STAT3hasbeenstudiedasatumortherapeutictarget.ThelastapproachusingsmallmoleculeSTAT3inhibitorshasbeenthemostexaminedsoHeterocylesandCarbazole.Heterocylesareanessentialclassofmolecules,assumingaroleinmanyaspectofourlife.Indeedheterocyclicnucleusisacommonfeatureofseveralbiomoleculeandbioactivecompoundsincludingagrochemicalproductsanddrugs.Inthisreviewwefocusedontwoimportantclassofheterocycliccompounds:carbazolesandNHCs(N-heterocycliccarbenes)andthereimplicationsincancerinhibitions.Carbazoles,prevalentasstructuralmotifsinvarioussyntheticmaterialsandnaturallyoccurringalkaloids,asisknown,havemanyapplicationsespeciallyaspromisingbioactivecompoundsduetotheirbiologicalproperties,knownsince1965.FurthermoreNHCsareaclassofstablecarbenesthatoverthelastfewyearshaveenteredthefieldas“new”ligandsforbioactivecoordinationcompounds.IthasbeendemonstratedthatmetalNHCcomplexescanbeusedtodevelophighlyefficientmetalbaseddrugswithpossibleapplicationsinthetreatmentofcancerorinfectiousdiseases.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
