Raf kinase inhibitor

Raf kinase inhibitor. High-throughput screening of a chemical collection at the former Bayer Research Center turned up... 

Fig. 1.15. Contrasting raf kinase inhibitor optimization strategies (reprinted ( adapted or in part ) with permission from Journal of Vie American Chemical Society. Copyright 2002 American Chemical Society).

S., WaUing, T., Wild, H. (2001) Discovery of heterocyclic ureas as a new class of raf kinase inhibitors identification of a second generation lead by a combinatorial chemistry approach. Bioorg Med Chem Lett 11, 2775-2778. 

Lorenz K, Lohse MJ, Quitterer U (2003) Protein kinase C switches the Raf kinase inhibitor from Raf-1 to GRK-2. Nature 426(6966) 574-579... 

Smith, R. A., Barbosa, J., Blum, C. L., Bobko, M. A., Caringal, Y. V., Dally, R., et al. Discovery of Heterocyclic Ureas as a New Class of Raf Kinase Inhibitors Identification of a Second Generation Lead by a Combinatorial Chemistry Approach. Bioorg. Med. Chem. Lett. 2001,11, 2775-2778. 

Mross K, Steinbild S, Baas F, Reil H Buss P, Mersmann S, Voliotis D, Schwartz B, Brendel E. Drug-dnig interaction pharmacokinetic study with the Raf kinase inhibitor (RKI) BAY 43-9006 administered in combination with irinotecan (CPT-11) in patients widi solid tumors. Int J ClinPharmacol 77i r(2003) 41,618-19. 

Synthesis and designing aspects of coumarin derivatives as monoamine conformation-specific effects of Raf kinase inhibitors 12JMC7332. Current landscape of phosphodiesterase lOA (PDEIOA) inhibition 12JMC7299. 

Another Raf kinase inhibitor, sunitinib (Sutent), was approved in 2006 based on a multi-center, international randomized trial enrolling 750 patients with treatment-naive metastatic renal cell carcinoma (Motzer et al. 2007). In that study, patients were randomized to receive either Sutent or interferon-a (IFN-a). Common metastatic sites included lung, lymph nodes, bone, and liver. There were 96 events (25.6%) of progression/death on Sutent compared with 154 events (41.1%) on IFN-a. Median progression-free survival was 47.3 weeks for Sutent-treated patients and 22.0 weeks for patients treated with IFN. Objective response rate on the Sutent arm was 27.5 vs 5.3% on IFN-a arm. 

Baritaki, S., Katsman, A., Chatterjee, D., Yeung, K.C., Spandidos, D.A., and Bonavida, B. (2007b). Regulation of tumor cell sensitivity to TRAlL-induced apoptosis by the metastatic suppressor Raf kinase inhibitor protein via Yin Yang 1 inhibition and death receptor 5 up-regulation. J. Immunol. 179, 5441-5453. 

Fu, Z., Kitagawa, Y, Shen, R., Shah, R., Mehra, R., Rhodes, D., Keller, P.J., Mizokami, A., Dunn, R., Chinnaiyan, A.M., et al. (2006). Metastasis suppressor gene Raf kinase inhibitor protein (RKIP) is a novel prognostic marker in prostate cancer. Prostate. 66, 248-256. 

Schuierer, M.M., BataiUe, F., Hagan, S., Kolch, W., and Bosserhoff, A.K. (2004). Reduction in Raf kinase inhibitor protein expression is associated with increased Ras-extraceUular signal-regulated kinase signaling in melanoma cell lines. Cancer Res. 64,5186-5192. 

B., Wyche, J., Kolch, W, and Sedivy, J.M. (2001). Raf kinase inhibitor protein interacts with NF-kappaB-inducing kinase and TAKl and inhibits NF-kappaB activation. Mol. Cell Biol. 21, 7207-7217. 

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