Kinase Inhibitor Drugs (Wiley Series in Drug Discovery and by Rongshi Li, Jeffrey A. Stafford

By Rongshi Li, Jeffrey A. Stafford

A accomplished source on case stories of advertised kinase medicinal drugs and promising drug trialsSince the invention of protein kinase task in 1954, the sphere of protein kinase drug discovery has complicated dramatically. With the continuing medical good fortune of the Bcr-Abl kinase inhibitor Gleevec within the remedy of power myelogenous leukemia and 7 extra advertised kinase inhibitor medications, researchers have compelling proof that kinase inhibitors may be hugely efficacious within the therapy of ailments attributable to aberrant job of protein kinase. at the moment greater than a hundred protein kinase inhibitors are in scientific development.In one entire quantity, the editors, Dr. Rongshi Li and Dr. Jeffrey Stafford, current well timed and demanding case reports of advertised kinase medications and several other of the main complicated kinase inhibitors in scientific trials. Kinase Inhibitor medications includes:Case reports from major investigators and specialists within the box that offer firsthand debts of kinase inhibitor discoveryCurrent considering on kinase constitution, biochemistry, and sign transduction pathwaysInformation on state of the art applied sciences and instruments reminiscent of structure-based and fragment-based drug discoveryA lineup of clinical-phase development issue receptor inhibitorsInhibitors of phone cycle kinasesThe discovery of allosteric inhibitors of MEK kinaseInformation on pharmacogenomics and its software to kinase inhibitor medical improvement

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2006). Effects of SU11248, a class III and V receptor tyrosine kinase inhibitor, on GIST-T1 cells: enhancement of growth inhibition via inhibition of PI3K/Akt/mTOR signaling. Cancer Sci. 97, 945–951. REFERENCES 37 Kim, K. , et al. (1993). Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumor growth in vivo. Nature. 362, 841–844. Kim, W. , and Kaelin, W. G. Jr. (2006). Molecular pathways in renal cell carcinoma— rationale for targeted treatment. Semin Oncol. 33, 588–595.

2003). In vivo anti-tumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 9, 327–337. , Shawver, L. , Plate, K. , et al. (1994). Glioblastoma growth inhibited in vivo by a dominant-negative Flk-1 mutant. Nature. 367, 576–579. , Longhi, M. , Plate, K. , et al. (1996). Dominant-negative inhibition of Flk-1 suppresses the growth of many tumor types in vivo.

2003) helped build confidence in clinical trial results. In the clinical setting, a dose-ranging pharmacokinetic trial of patients with advanced solid tumors identified 50 mg/ day (administered in 6 week treatment cycles of 4 weeks on and 2 weeks off) as the recommended SU11248 dose. , 2006). This trial achieved a mean steady-state plasma level of 125 ng/mL and supported further studies since this plasma level exceeded the minimum target plasma levels required in animal efficacy studies. Significant additional clinical studies focused on inhibition of RTK targets with an attempt to link target inhibition with SU11248 plasma levels.

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