Imatinib: a selective tyrosine kinase inhibitor.

摘要: The understanding of the pathophysiology a large number cancer types provides strategy to target cells with minimal effect on normal cells. Protein phosphorylation and dephosphorylation play pivotal role in intracellular signaling; regulate signal transduction pathways, there are approximately 700 protein kinases 100 phosphatases encoded within human genome. In cancer, as well other proliferative diseases, unregulated cell proliferation, differentiation survival frequently results from abnormal phosphorylation. Although it is often possible identify single kinase that plays given disease, development drugs based upon inhibition has been hampered by unacceptable side effects resulting lack selectivity. With growing molecular biology tyrosine use structural information, design potential directed towards bind adenosine triphosphate (ATP)-binding site become possible. These advances have transferred emphasis away identification potent inhibitors more issues selectivity, cellular efficacy, therapeutic effectiveness tolerability. this paper, relationship between drug discovery methods, utilized for anticancer drugs, will be illustrated.