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Items: 17

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.

Cancer Cell. 2012 Jul 10;22(1):51-65. doi: 10.1016/j.ccr.2012.05.019.

2.

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.

ACS Med Chem Lett. 2012 May 8;3(7):602-6. doi: 10.1021/ml300110s. eCollection 2012 Jul 12.

3.

Combined inhibition of EGFR and CK2 augments the attenuation of PI3K-Akt-mTOR signaling and the killing of cancer cells.

Bliesath J, Huser N, Omori M, Bunag D, Proffitt C, Streiner N, Ho C, Siddiqui-Jain A, O'Brien SE, Lim JK, Ryckman DM, Anderes K, Rice WG, Drygin D.

Cancer Lett. 2012 Sep 1;322(1):113-8. doi: 10.1016/j.canlet.2012.02.032. Epub 2012 Mar 2.

PMID:
22387988
4.

Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.

Haddach M, Michaux J, Schwaebe MK, Pierre F, O'Brien SE, Borsan C, Tran J, Raffaele N, Ravula S, Drygin D, Siddiqui-Jain A, Darjania L, Stansfield R, Proffitt C, Macalino D, Streiner N, Bliesath J, Omori M, Whitten JP, Anderes K, Rice WG, Ryckman DM.

ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. doi: 10.1021/ml200259q. eCollection 2012 Feb 9.

5.

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.

Mol Cancer Ther. 2012 Apr;11(4):994-1005. doi: 10.1158/1535-7163.MCT-11-0613. Epub 2012 Jan 20.

6.

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.

Biochem Biophys Res Commun. 2011 Nov 11;415(1):163-7. doi: 10.1016/j.bbrc.2011.10.046. Epub 2011 Oct 18.

PMID:
22027148
7.

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.

Mol Cell Biochem. 2011 Oct;356(1-2):37-43. doi: 10.1007/s11010-011-0956-5. Epub 2011 Jul 14.

PMID:
21755459
8.

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.

J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21.

PMID:
21174434
9.

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.

Cancer Res. 2011 Feb 15;71(4):1418-30. doi: 10.1158/0008-5472.CAN-10-1728. Epub 2010 Dec 15.

10.

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.

Cancer Res. 2010 Dec 15;70(24):10288-98. doi: 10.1158/0008-5472.CAN-10-1893.

11.

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.

Cancer Res. 2009 Oct 1;69(19):7653-61. doi: 10.1158/0008-5472.CAN-09-1304. Epub 2009 Sep 8.

12.

A method for detecting and preventing negative RNA interference in preparation of lentiviral vectors for siRNA delivery.

Zhou D, Zhang J, Wang C, Bliesath JR, He Q, Yu D, Li-He Z, Wong-Staal F.

RNA. 2009 Apr;15(4):732-40. doi: 10.1261/rna.985209. Epub 2009 Feb 25.

13.

Structural and biochemical characterization of the therapeutic Anabaena variabilis phenylalanine ammonia lyase.

Wang L, Gamez A, Archer H, Abola EE, Sarkissian CN, Fitzpatrick P, Wendt D, Zhang Y, Vellard M, Bliesath J, Bell SM, Lemontt JF, Scriver CR, Stevens RC.

J Mol Biol. 2008 Jul 18;380(4):623-35. doi: 10.1016/j.jmb.2008.05.025. Epub 2008 May 17.

14.

Generation of shRNA pool library: a revision of the biological technique from the viewpoint of chemistry.

Zhou D, Wang C, Zhang J, Bliesath J, He QS, Ke N, Yu D, Li Q, Zhang LH, Wong-Staal F.

Chembiochem. 2008 Jun 16;9(9):1365-7. doi: 10.1002/cbic.200800049. No abstract available.

PMID:
18435449
15.

A more efficient RNAi inducible system for tight regulation of gene expression in mammalian cells and xenograft animals.

Zhang J, Wang C, Ke N, Bliesath J, Chionis J, He QS, Li QX, Chatterton JE, Wong-Staal F, Zhou D.

RNA. 2007 Aug;13(8):1375-83. Epub 2007 Jul 6.

16.

A novel RNAi library based on partially randomized consensus sequences of nuclear receptors: identifying the receptors involved in amyloid beta degradation.

Yang JP, Fan W, Rogers C, Chatterton JE, Bliesath J, Liu G, Ke N, Wang CY, Rhoades K, Wong-Staal F, Li QX.

Genomics. 2006 Sep;88(3):282-92. Epub 2006 May 2.

17.

A 96-well surrogate survival assay coupled with a special short interfering RNA vector for assessing cancer gene targets with enhanced signal/noise ratio and its utility in HTS for cancer therapeutic targets.

Yu DH, Chatterton JE, Bliesath JR, Sundaram R, Ke N, Nguy V, Meyhack B, Wong-Staal F, Li QX.

Assay Drug Dev Technol. 2005 Aug;3(4):401-11.

PMID:
16180995

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