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A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation)... We describe the molecular structure and classication of tyrosine kinase inhibitors, their mechanism of action, and their inhibitory activity against specic kinase signaling Mechanism of Action (Imatinib) Mechanism of Action (Nilotinib) - Nilotinib is a potent and selective inhibitor of tyrosine kinase of the BCRABL , It binds strongly with ATP-binding site . - It is a potent inhibitor of wild- type... 10. BCR-ABL Tyrosine Kinase Inhibitors• Mechanism of action :• IMATINIB & NILOTINIB: bind to a segment of the kinase domain that fixes the enzyme in a closed or nonfunctional state, in which the protein is unable to bind its substrate/phosphate donor, ATP.• "These groups of agents in addition to inhibiting the synthesis of angiogenic factors can inhibit several other aspects of cancer biology such as growth, resistance to apoptosis or metastasis. Agents that target the angiogenic receptors are mainly tyrosine kinase inhibitors (sorafenib, sunitinib, pazopanib... Three anti-angiogenic tyrosine kinase inhibitors (TKIs), sunitinib, sorafenib and pazopanib, with differential binding capacities to angiogenic Three Anti-Angiogenic tyrosine kinase inhibitors (TKIs), sunitinib, sorafenib and pazopanib, with differential binding capacities to angiogenic CML or GIST tyrosine kinase inhibitors. Mechanism of action for imatininb. Those are thought to contribute to the side-effect prole of BCR-ABL tyrosine kinase inhibitors. Imatinib mesylate is a small-molecule tyrosine kinase inhibitor that was initially developed as a 2-phenylaminopyrimidine derivative specific for PDGFR. Информация взята v3.kz |
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