Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Michael K. Schwaebe"'
Autor:
William G. Rice, Kenna Anderes, David Ryckman, Ross D. Hannan, Megan J. Bywater, Elaine Sanij, Jaclyn E. Quin, Nicole Streiner, Adam Siddiqui-Jain, Michael K. Schwaebe, Mustapha Haddach, Mayuko Omori, Chris Proffitt, Sean E. O'Brien, Caroline B. Ho, Josh Bliesath, Amy Lin, Denis Drygin
Supplementary Materials from Targeting RNA Polymerase I with an Oral Small Molecule CX-5461 Inhibits Ribosomal RNA Synthesis and Solid Tumor Growth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c0b64b9899bae18205e730a978712b0
https://doi.org/10.1158/0008-5472.22387916.v1
https://doi.org/10.1158/0008-5472.22387916.v1
Autor:
Kenna Anderes, William G. Rice, David M. Ryckman, Michael K. Schwaebe, Chris Proffitt, Caroline Ho, Nanni Huser, Mayuko Omori, Josh Bliesath, Sean E. O'Brien, Fabrice Pierre, Peter Chua, Nicole Streiner, Denis Drygin, Adam Siddiqui-Jain
Supplementary Methods from CX-4945, an Orally Bioavailable Selective Inhibitor of Protein Kinase CK2, Inhibits Prosurvival and Angiogenic Signaling and Exhibits Antitumor Efficacy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c5cc2abcc1fc3202335d6528f4c2a9a
https://doi.org/10.1158/0008-5472.22386579
https://doi.org/10.1158/0008-5472.22386579
Autor:
Kenna Anderes, William G. Rice, David M. Ryckman, Michael K. Schwaebe, Chris Proffitt, Caroline Ho, Nanni Huser, Mayuko Omori, Josh Bliesath, Sean E. O'Brien, Fabrice Pierre, Peter Chua, Nicole Streiner, Denis Drygin, Adam Siddiqui-Jain
Malignant transformation and maintenance of the malignant phenotype depends on oncogenic and non-oncogenic proteins that are essential to mediate oncogene signaling and to support the altered physiologic demands induced by transformation. Protein kin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1119ad46a45018a2830b6d70f1b000dd
https://doi.org/10.1158/0008-5472.c.6501576
https://doi.org/10.1158/0008-5472.c.6501576
Autor:
Jeffrey P. Whitten, Ryan Stansfield, Chris Proffitt, Adam Siddiqui-Jain, Johnny Y. Nagasawa, Josh Bliesath, Pauline Kerdoncuff, Kenna Anderes, David M. Ryckman, Nanni Huser, May Omori, Levan Darjania, William G. Rice, Mustapha Haddach, Denis Drygin, Jerome Michaux, Michael K. Schwaebe, Fabrice Pierre, Sean O'Brien
Publikováno v:
ACS Medicinal Chemistry Letters. 3:602-606
Accelerated proliferation of solid tumor and hematologic cancer cells is linked to accelerated transcription of rDNA by the RNA polymerase I (Pol I) enzyme to produce elevated levels of rRNA (rRNA). Indeed, upregulation of Pol I, frequently caused by
Autor:
Fabrice Pierre, Collin F. Regan, David M. Ryckman, Mustapha Haddach, Michael K. Schwaebe, Michael E. Jung
Publikováno v:
Synlett. 23:443-447
This paper reports the synthesis of various 5-halopyrimidine-4-carboxylic acid esters via the Minisci homolytic alkoxycarbonylation of 5-halopyrimidines. The reaction was found to be highly regioselective, allowing the one-step synthesis of useful am
Autor:
Denis Drygin, Jerome Michaux, Fabrice Pierre, Diwata Macalino, Mustapha Haddach, Cosmin Borsan, David M. Ryckman, Collin F. Regan, Sean O'Brien, Pauline Kerdoncuff, Eric Stefan, Adam Siddiqui-Jain, Peter C. Chua, Michael K. Schwaebe, William G. Rice
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:45-48
Protein kinase CK2 is a potential drug target for many diseases including cancer and inflammation disorders. The crystal structure of clinical candidate CX-4945 1 with CK2 revealed an indirect interaction with the protein through hydrogen bonding bet
Autor:
Chris Proffitt, Johnny Y. Nagasawa, Levan Darjania, Eric Stefan, Ryan Stansfield, Sean O'Brien, Nicole Streiner, Jeffrey P. Whitten, Joshua R. Bliesath, Peter C. Chua, Caroline B. Ho, Pauline Bourbon, William G. Rice, Fabrice Pierre, Adam Siddiqui-Jain, Ta Kung Chen, Kenna Anderes, Anne Vialettes, Mustapha Haddach, David M. Ryckman, Michael K. Schwaebe, Denis Drygin, Jerome Michaux, May Omori
Publikováno v:
Molecular and Cellular Biochemistry. 356:37-43
In this article we describe the preclinical characterization of 5-(3-chlorophenylamino) benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first orally available small molecule inhibitor of protein CK2 in clinical trials for cancer. CX-4945
Autor:
Johnny Y. Nagasawa, Michael K. Schwaebe, Fabrice Pierre, Mustapha Haddach, Anne Vialettes, David M. Ryckman
Publikováno v:
Tetrahedron Letters. 52:1096-1100
Quinolone esters are readily converted into the corresponding amides using aluminum chloride at room temperature in excellent yields and purities. The method is both general and scalable to multi-kilogram quantities.
Autor:
Caroline B. Ho, Daniel D. Von Hoff, Denis Drygin, Chris Proffitt, Jeffrey P. Whitten, Kenna Anderes, William G. Rice, Josh Bliesath, Amy M. Lin, John K.C. Lim, Katy Trent, Sean O'Brien, Michael K. Schwaebe, Adam Siddiqui-Jain
Publikováno v:
Cancer Research. 69:7653-7661
Hallmark deregulated signaling in cancer cells drives excessive ribosome biogenesis within the nucleolus, which elicits unbridled cell growth and proliferation. The rate-limiting step of ribosome biogenesis is synthesis of rRNA (building blocks of ri
Autor:
Peter C. Chua, Michael K. Schwaebe, Johnny Y. Nagasawa, Anne Vialettes, Jeffrey P. Whitten, Fabrice Pierre
Publikováno v:
Tetrahedron Letters. 49:4437-4442
A novel and efficient synthesis of 5-oxo-6-carboxy-naphthyridines is reported in this Letter along with a discussion of scope and limitations. Activated 3-nicotinic acids readily acylate the magnesium anion of 2-(benzothiazol-2-yl) or 2-(benzimidazol