The RNA polymerase I transcription machinery: an emerging target for the treatment of cancerDenis Drygin
Cylene Pharmaceuticals, San Diego, California, USA
Annu Rev Pharmacol Toxicol 50:131-56. 2010
..In this review, we discuss experimental data and potential strategies to downregulate rRNA synthesis and induce an antiproliferative response in cancer cells...
- Protein kinase CK2 modulates IL-6 expression in inflammatory breast cancer
Denis Drygin
Cylene Pharmaceuticals, 5820 Nancy Ridge Dr Ste 200, San Diego, CA 92121, USA
Biochem Biophys Res Commun 415:163-7. 2011
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- Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth
Denis Drygin
Cylene Pharmaceuticals, Inc, San Diego, California, USA
Cancer Res 71:1418-30. 2011
..Our findings position CX-5461 for investigational clinical trials as a potent, selective, and orally administered agent for cancer treatment...
- Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer
Fabrice Pierre
Cylene Pharmaceuticals, San Diego, CA 92121, USA
Mol Cell Biochem 356:37-43. 2011
..In vivo time-dependent reduction in the phosphorylation of the biomarker p21 at T145 was observed by immunohistochemistry. Inhibition of the newly validated CK2 target by CX-4945 represents a fresh therapeutic strategy for cancer...
- 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity
Fabrice Pierre
Cylene Pharmaceuticals, 5820 Nancy Ridge Drive, Suite 200, San Diego, CA 92121, USA
Bioorg Med Chem Lett 21:6687-92. 2011
..This work delivers an excellent lead-optimization platform for Pim targeting anticancer therapies...
- Anticancer activity of CX-3543: a direct inhibitor of rRNA biogenesis
Denis Drygin
Cylene Pharmaceuticals, Inc, San Diego, CA 92121, USA
Cancer Res 69:7653-61. 2009
..CX-3543 is the first G-quadruplex interactive agent to enter human clinical trials, and it is currently under evaluation against carcinoid/neuroendocrine tumors in a phase II clinical trial...
- Synthesis and SAR of inhibitors of protein kinase CK2: novel tricyclic quinoline analogs
Mustapha Haddach
Cylene Pharmaceuticals Inc, 5820 Nancy Ridge Drive, Suite 200, San Diego, CA 92121, USA
Bioorg Med Chem Lett 22:45-8. 2012
..Herein, we investigate the relevance of this hydrogen bond by preparing several novel tricyclic derivatives lacking a NH moiety at the same position. This SAR study allowed the discovery of highly potent CK2 inhibitors...
- 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
Fabrice Pierre
Cylene Pharmaceuticals, 5820 Nancy Ridge Drive, Suite 200, San Diego, California 92121, United States
J Med Chem 54:635-54. 2011
..25n was found to be highly selective, orally bioavailable across species (20-51%) and efficacious in xenograft models. The discovery of 25n will allow the therapeutic targeting of CK2 in humans for the first time...
- CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy
Adam Siddiqui-Jain
Cylene Pharmaceuticals, 5820 Nancy Ridge Drive, Suite 200, San Diego, CA 92121, USA
Cancer Res 70:10288-98. 2010
..Finally, CX-4945 is the first orally bioavailable small molecule inhibitor of CK2 to advance into human clinical trials, thereby paving the way for an entirely new class of targeted treatment for cancer...
