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Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives
- Publication Year :
- 2014
-
Abstract
- 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.
- Subjects :
- Clinical Biochemistry
Fusion Proteins, bcr-abl
Pharmaceutical Science
Apoptosis
Biochemistry
Settore MED/15 - Malattie Del Sangue
Cell Line
Structure-Activity Relationship
Pimozide
Settore BIO/13 - Biologia Applicata
hemic and lymphatic diseases
Drug Discovery
medicine
STAT5 Transcription Factor
Cytotoxic T cell
Humans
Phosphorylation
Molecular Biology
Transcription factor
STAT5
Cell Proliferation
biology
Dose-Response Relationship, Drug
Molecular Structure
Chemistry
STAT5 inhibitors,Pimozide,BCR/ABL expressing leukemia, Apoptosis,Cell growth inhibition
Organic Chemistry
Cell Cycle
medicine.disease
Settore CHIM/08 - Chimica Farmaceutica
Leukemia
Cancer research
biology.protein
Settore BIO/14 - Farmacologia
Molecular Medicine
K562 Cells
medicine.drug
Chronic myelogenous leukemia
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....7fa867092888c9d300fda9c3935447bd