- Utility of Clinical Biomarkers for Detecting Protein Kinase CK2 Inhibition: A Report from the Phase I Trial of CX-4945
April 2010
View Poster
- Phase I Clinical Trial of CX-4945: A First-in-Class, Orally Administered Small Molecule Inhibitor of Protein Kinase CK2
November 2009
View Poster
- CX-4945, a Novel Small Molecule Inhibitor of CK2 Protein Kinase, Reduces Hyperactivated AKT Signaling and Synergizes with AKT Inhibitors in Breast Cancer Cells
November 2009
View Poster
- Discovery of Selective Small Molecule Pan-Pim Kinase Inhibitors with Potent Oral Efficacy in Murine Xenograft Models
November 2009
View Poster
- Discovery and Characterization of CX-4945, a Selective Orally Bioavailable Small Molecule Inhibitor of Protein Kinase CK2: Phase 1 Initiated
April 2009
View Poster
- CX-4945, a Small Molecule Inhibitor of CK2, Inhibits Angiogenesis by Affecting the Vascular Endothelium and Suppressing Hypoxia-Activated Hif-1 Alpha Transcription
April 2009
View Poster
- Quarfloxin (CX-3543) Phase I Clinical Data and Scientific Findings Supporting the Selection of Carcinoid/Neuroendocrine Tumors as the Phase II Indication
April 2009
View Poster
- CX-4945 Blocks the “Master Regulator CK2” in Multiple Intracellular Signaling Pathways Revealing Significant Anti-Proliferative and Anti-Tumor Activities
November 2008
View Poster
- CX-5461 a Novel, Orally Bioavailable and Selective Small Molecule Inhibitor of RNA Polymerase I Transcription Induces Autophagy and Shows Potent Anti-tumor Activity
October 2008
View Poster
- Discovery and Characterization of CX-5011, a Potent, Highly Selective, Oral Small Molecule Inhibitor of Protein Kinase CK2
April 2008
View Poster
- Quarfloxin (CX-3543) Disrupts the Nucleolin/ rDNA Quadruplex Complexes, Inhibits the Elongation by RNA Polymerase I and Exhibits Potent Antitumor Activity in Models of Cancer
April 2008
View Poster
- CX-5461 Selectively Inhibits SL1 Function of RNA Polymerase I Transcription in the Ribosome Biogenesis Pathway and Exhibits Potent Antitumor Activity in Cancer Models
April 2008
View Poster
|
Protein kinase CK2
Guerra B, Issinger OG. "Protein kinase CK2 in human diseases." Curr Med Chem. 2008;15(19):1870-86.
Sarno S, Pinna LA. "Protein kinase CK2 as a druggable target." Mol Biosyst. 2008 Sep;4(9):889-94.
Trembley JH, Wang G, Unger G, Slaton J, Ahmed K. "Protein kinase CK2 in health and disease: CK2: a key player in cancer biology." Cell Mol Life Sci. 2009 Jun;66(11-12):1858-67.
rRNA Biogenesis and Nucleolar Function
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. "Anticancer activity of CX-3543: a direct inhibitor of rRNA biogenesis." Cancer Res. 2009 Oct 1;69(19):7653-61.
Drygin D, Rice WG, Grummt I. "The RNA polymerase I transcription machinery: an emerging target for the treatment of cancer." Annu Rev Pharmacol Toxicol. 2010;50:131-56.
Burger K, Mühl B, Harasim T, Rohrmoser M, Malamoussi A, Orban M, Kellner M, Gruber-Eber A, Kremmer E, Hölzel M, Eick D. "Chemotherapeutic drugs inhibit ribosome biogenesis at various levels." J Biol Chem. 2010 Feb 18.
White RJ. "RNA polymerases I and III, growth control and cancer." Nat Rev Mol Cell Biol. 2005 Jan;6(1):69-78
Russell J, Zomerdijk JC. "RNA-polymerase-I-directed rDNA transcription, life and works." Trends Biochem Sci. 2005 Feb;30(2):87-96
|
