Philadelphia (Ph) chromosome is the cytogenetic hallmark of chronic myeloid leukemia (CML). The translocation forms a chimeric gene, bcr-abl, which generates BCR-ABL. This fusion protein constitutively activate ABL tyrosine kinase and causes CML. Imatinib mesylate is a selective tyrosine kinase inhibitor on ABL, c-Kit and PGDF-receptor, and functions through competitive inhibition at the ATP-binding site of the enzyme, which leads to growth arrest or apoptosis in cells that express BCR-ABL. Imatinib has revolutionized the management of patients with CML, and at a dose of 400 mg daily has become the current standard therapy for newly diagnosed patients with CML even when they have HLA-matched family donors. Although imatinib therapy has only a 5-year history, it is hoped that CML will be cured with this drug and with forthcoming second-generation tyrosine kinase inhibitors as well as by allogeneic stem cell transplantation in patients who have become resistant to these drugs.
Philadelphia ( Ph ) chromosome is the cytogenetic hallmark of chronic myeloid leukemia ( CML ) . The translocation forms a chimeric gene , bcr - abl , which generates BCR - ABL . This fusion protein constitutively activate ABL tyrosine kinase and causes CML . Imatinib mesylate is a selective tyrosine kinase inhibitor on ABL , c - Kit and PGDF - receptor , and functions through competitive inhibition at the ATP - binding site of the enzyme , which leads to growth arrest or apoptosis in cells that express BCR - ABL . Imatinib has revolutionized the management of patients with CML , and at a dose of 400 mg daily has become the current standard therapy for newly diagnosed patients with CML even when they have HLA - matched family donors . Although imatinib therapy has only a 5-year history , it is hoped that CML will be cured with this drug and with forthcoming second - generation tyrosine kinase inhibitors as well as by allogeneic stem cell transplantation in patients who have become resistant to these drugs .
What tyrosine kinase, involved in a Philadelphia- chromosome positive chronic myelogenous leukemia, is the target of Imatinib (Gleevec)?
What tyrosine kinase , involved in a Philadelphia- chromosome positive chronic myelogenous leukemia , is the target of Imatinib ( Gleevec ) ?
BCR-ABL
BCR-ABL