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Page 1
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B, Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M, Friedman LS, Malek S. Hatzivassiliou G, et al. Nature. 2010 Mar 18;464(7287):431-5. doi: 10.1038/nature08833. Epub 2010 Feb 3. Nature. 2010. PMID: 20130576
Discovery of pyrrolopyrimidine inhibitors of Akt.
Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ. Blake JF, et al. Among authors: morales th. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13. Bioorg Med Chem Lett. 2010. PMID: 20810279
Discovery and SAR of spirochromane Akt inhibitors.
Kallan NC, Spencer KL, Blake JF, Xu R, Heizer J, Bencsik JR, Mitchell IS, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ. Kallan NC, et al. Among authors: morales th. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21392984
Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.
Xu R, Banka A, Blake JF, Mitchell IS, Wallace EM, Bencsik JR, Kallan NC, Spencer KL, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ. Xu R, et al. Among authors: morales th. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26. Bioorg Med Chem Lett. 2011. PMID: 21420856
Potent and selective pyrazole-based inhibitors of B-Raf kinase.
Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A. Hansen JD, et al. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. doi: 10.1016/j.bmcl.2008.07.002. Epub 2008 Jul 5. Bioorg Med Chem Lett. 2008. PMID: 18676143
Non-oxime inhibitors of B-Raf(V600E) kinase.
Ren L, Wenglowsky S, Miknis G, Rast B, Buckmelter AJ, Ely RJ, Schlachter S, Laird ER, Randolph N, Callejo M, Martinson M, Galbraith S, Brandhuber BJ, Vigers G, Morales T, Voegtli WC, Lyssikatos J. Ren L, et al. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1243-7. doi: 10.1016/j.bmcl.2010.12.061. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21251822
The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.
Buckmelter AJ, Ren L, Laird ER, Rast B, Miknis G, Wenglowsky S, Schlachter S, Welch M, Tarlton E, Grina J, Lyssikatos J, Brandhuber BJ, Morales T, Randolph N, Vigers G, Martinson M, Callejo M. Buckmelter AJ, et al. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1248-52. doi: 10.1016/j.bmcl.2010.12.039. Epub 2010 Dec 10. Bioorg Med Chem Lett. 2011. PMID: 21211972
Non-oxime pyrazole based inhibitors of B-Raf kinase.
Newhouse BJ, Hansen JD, Grina J, Welch M, Topalov G, Littman N, Callejo M, Martinson M, Galbraith S, Laird ER, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A. Newhouse BJ, et al. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3488-92. doi: 10.1016/j.bmcl.2010.12.038. Epub 2010 Dec 17. Bioorg Med Chem Lett. 2011. PMID: 21536432
29 results