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Page 1
Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53.
Bywater MJ, Poortinga G, Sanij E, Hein N, Peck A, Cullinane C, Wall M, Cluse L, Drygin D, Anderes K, Huser N, Proffitt C, Bliesath J, Haddach M, Schwaebe MK, Ryckman DM, Rice WG, Schmitt C, Lowe SW, Johnstone RW, Pearson RB, McArthur GA, Hannan RD. Bywater MJ, et al. Among authors: anderes k. Cancer Cell. 2012 Jul 10;22(1):51-65. doi: 10.1016/j.ccr.2012.05.019. Cancer Cell. 2012. PMID: 22789538 Free PMC article.
Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth.
Drygin D, Lin A, Bliesath J, Ho CB, O'Brien SE, Proffitt C, Omori M, Haddach M, Schwaebe MK, Siddiqui-Jain A, Streiner N, Quin JE, Sanij E, Bywater MJ, Hannan RD, Ryckman D, Anderes K, Rice WG. Drygin D, et al. Among authors: anderes k. Cancer Res. 2011 Feb 15;71(4):1418-30. doi: 10.1158/0008-5472.CAN-10-1728. Epub 2010 Dec 15. Cancer Res. 2011. PMID: 21159662
Anticancer activity of CX-3543: a direct inhibitor of rRNA biogenesis.
Drygin D, Siddiqui-Jain A, O'Brien S, Schwaebe M, Lin A, Bliesath J, Ho CB, Proffitt C, Trent K, Whitten JP, Lim JK, Von Hoff D, Anderes K, Rice WG. Drygin D, et al. Among authors: anderes k. Cancer Res. 2009 Oct 1;69(19):7653-61. doi: 10.1158/0008-5472.CAN-09-1304. Epub 2009 Sep 8. Cancer Res. 2009. PMID: 19738048
CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy.
Siddiqui-Jain A, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C, Proffitt C, Schwaebe MK, Ryckman DM, Rice WG, Anderes K. Siddiqui-Jain A, et al. Among authors: anderes k. Cancer Res. 2010 Dec 15;70(24):10288-98. doi: 10.1158/0008-5472.CAN-10-1893. Cancer Res. 2010. PMID: 21159648
Protein kinase CK2 modulates IL-6 expression in inflammatory breast cancer.
Drygin D, Ho CB, Omori M, Bliesath J, Proffitt C, Rice R, Siddiqui-Jain A, O'Brien S, Padgett C, Lim JK, Anderes K, Rice WG, Ryckman D. Drygin D, et al. Among authors: anderes k. Biochem Biophys Res Commun. 2011 Nov 11;415(1):163-7. doi: 10.1016/j.bbrc.2011.10.046. Epub 2011 Oct 18. Biochem Biophys Res Commun. 2011. PMID: 22027148
CK2 inhibitor CX-4945 suppresses DNA repair response triggered by DNA-targeted anticancer drugs and augments efficacy: mechanistic rationale for drug combination therapy.
Siddiqui-Jain A, Bliesath J, Macalino D, Omori M, Huser N, Streiner N, Ho CB, Anderes K, Proffitt C, O'Brien SE, Lim JK, Von Hoff DD, Ryckman DM, Rice WG, Drygin D. Siddiqui-Jain A, et al. Among authors: anderes k. Mol Cancer Ther. 2012 Apr;11(4):994-1005. doi: 10.1158/1535-7163.MCT-11-0613. Epub 2012 Jan 20. Mol Cancer Ther. 2012. PMID: 22267551
Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics.
Haddach M, Schwaebe MK, Michaux J, Nagasawa J, O'Brien SE, Whitten JP, Pierre F, Kerdoncuff P, Darjania L, Stansfield R, Drygin D, Anderes K, Proffitt C, Bliesath J, Siddiqui-Jain A, Omori M, Huser N, Rice WG, Ryckman DM. Haddach M, et al. Among authors: anderes k. ACS Med Chem Lett. 2012 May 8;3(7):602-6. doi: 10.1021/ml300110s. eCollection 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 24900516 Free PMC article.
Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer.
Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Rice WG, Ryckman DM, Anderes K. Pierre F, et al. Among authors: anderes k. Mol Cell Biochem. 2011 Oct;356(1-2):37-43. doi: 10.1007/s11010-011-0956-5. Epub 2011 Jul 14. Mol Cell Biochem. 2011. PMID: 21755459
Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM. Pierre F, et al. Among authors: anderes k. J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21. J Med Chem. 2011. PMID: 21174434
37 results