6533b854fe1ef96bd12ae07d
RESEARCH PRODUCT
Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives.
Stefania GrimaudoRiccardo BaruchelloMaria MeliRiccardo RondaninRomeo RomagnoliManlio TolomeoPaolo MarchettiGiacomo PadroniSara FochiMaria Rosaria PipitoneDaniele SimoniCristiana Costantinisubject
Clinical BiochemistryFusion Proteins bcr-ablPharmaceutical ScienceApoptosisBiochemistrySettore MED/15 - Malattie Del SangueCell LineStructure-Activity RelationshipPimozideSettore BIO/13 - Biologia Applicatahemic and lymphatic diseasesDrug DiscoverymedicineSTAT5 Transcription FactorCytotoxic T cellHumansPhosphorylationMolecular BiologyTranscription factorSTAT5Cell ProliferationbiologyDose-Response Relationship DrugMolecular StructureChemistrySTAT5 inhibitorsPimozideBCR/ABL expressing leukemia ApoptosisCell growth inhibitionOrganic ChemistryCell CyclePimozidemedicine.diseaseSettore CHIM/08 - Chimica FarmaceuticaLeukemiaApoptosisCancer researchbiology.proteinSettore BIO/14 - FarmacologiaMolecular MedicinePhosphorylationK562 Cellsmedicine.drugChronic myelogenous leukemiadescription
STATs are transcription factors acting as intracellular signaling after stimulation with cytokines, growth factors and hormones. STAT5 is also constitutively active in many forms of cancers, including chronic myelogenous leukemia, acute lymphoblastic leukemia and Hodgkin's lymphoma. Recently, literature reported that the neuroleptic drug pimozide inhibits STAT5 phosphorylation inducing apoptosis in CML cells. We undertook an investigation from pimozide structure, obtaining simple derivatives with cytotoxic and STAT5-inhibitory activity, two of them markedly more potent than pimozide.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2014-01-01 |