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Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors.
Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, Patel BKR, Peek VL, Stephens JR, Stewart JA, Stout SL, Timm DE, Um SL, Willard MD, Wulur IH, Zeng Y, Wang Y, Walgren RA, Betty Yan SC. Konicek BW, et al. Oncotarget. 2018 Feb 13;9(17):13796-13806. doi: 10.18632/oncotarget.24488. eCollection 2018 Mar 2. Oncotarget. 2018. PMID: 29568395 Free PMC article.
LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models.
Yan SB, Peek VL, Ajamie R, Buchanan SG, Graff JR, Heidler SA, Hui YH, Huss KL, Konicek BW, Manro JR, Shih C, Stewart JA, Stewart TR, Stout SL, Uhlik MT, Um SL, Wang Y, Wu W, Yan L, Yang WJ, Zhong B, Walgren RA. Yan SB, et al. Among authors: konicek bw. Invest New Drugs. 2013 Aug;31(4):833-44. doi: 10.1007/s10637-012-9912-9. Epub 2012 Dec 29. Invest New Drugs. 2013. PMID: 23275061 Free PMC article. Clinical Trial.
Therapeutic inhibition of MAP kinase interacting kinase blocks eukaryotic initiation factor 4E phosphorylation and suppresses outgrowth of experimental lung metastases.
Konicek BW, Stephens JR, McNulty AM, Robichaud N, Peery RB, Dumstorf CA, Dowless MS, Iversen PW, Parsons S, Ellis KE, McCann DJ, Pelletier J, Furic L, Yingling JM, Stancato LF, Sonenberg N, Graff JR. Konicek BW, et al. Cancer Res. 2011 Mar 1;71(5):1849-57. doi: 10.1158/0008-5472.CAN-10-3298. Epub 2011 Jan 13. Cancer Res. 2011. PMID: 21233335
The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts.
Graff JR, McNulty AM, Hanna KR, Konicek BW, Lynch RL, Bailey SN, Banks C, Capen A, Goode R, Lewis JE, Sams L, Huss KL, Campbell RM, Iversen PW, Neubauer BL, Brown TJ, Musib L, Geeganage S, Thornton D. Graff JR, et al. Among authors: konicek bw. Cancer Res. 2005 Aug 15;65(16):7462-9. doi: 10.1158/0008-5472.CAN-05-0071. Cancer Res. 2005. PMID: 16103100
Therapeutic suppression of translation initiation factor eIF4E expression reduces tumor growth without toxicity.
Graff JR, Konicek BW, Vincent TM, Lynch RL, Monteith D, Weir SN, Schwier P, Capen A, Goode RL, Dowless MS, Chen Y, Zhang H, Sissons S, Cox K, McNulty AM, Parsons SH, Wang T, Sams L, Geeganage S, Douglass LE, Neubauer BL, Dean NM, Blanchard K, Shou J, Stancato LF, Carter JH, Marcusson EG. Graff JR, et al. Among authors: konicek bw. J Clin Invest. 2007 Sep;117(9):2638-48. doi: 10.1172/JCI32044. J Clin Invest. 2007. PMID: 17786246 Free PMC article.
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