Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Levan Darjania"'
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:
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:
Jeff Kucharski, Ulf Peters, Yun O. Long, Shisheng Li, Pingda Ren, Ata Zarieh, Dana D. Hu-Lowe, Ke Yu, Yuan Liu, Tao Wu, Carol Thach, Dirk Brehmer, Tess Ely, Xin Guo, Patrick P. Zarrinkar, Matthew P. Patricelli, Yi Wang, Rasmus Hansen, Dashyant Dhanak, Yi Liu, Jun Feng, Shuangwei Li, Matthew R. Janes, Yuching Chen, Sarah J. Firdaus, Levan Darjania, Linda Kessler, Jeffrey H. Chen, Xiaohu Deng, Yvonne Yao, Anjali Babbar, Matthew V. Lorenzi, Jingchuan Zhang, Lian-Sheng Li
Publikováno v:
Cell. 172:578-589.e17
KRASG12C was recently identified to be potentially druggable by allele-specific covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP). Success of this approach requires active cycling of KRASG12C between its act
Autor:
Hidetoshi Okuyama, Takashi Okamoto, Guy A. Thompson, Nobutoshi Ichise, Satoko Ichikawa, Levan Darjania
Publikováno v:
Plant Physiology and Biochemistry. 40:69-79
Arabinogalactan proteins (AGPs) are very large proteoglycans thought to have more of a signaling than a structural role when secreted into the plant cell wall. AGPs are also the first known family of abundant plant proteins synthesized with glycosylp
Autor:
Shuangwei Li, Jingchuan Zhang, Linda Kessler, Ata Zarieh, Pingda Ren, Yi Wang, Carol Thach, Tao Wu, Yvonne Yao, Lian-Sheng Li, Yi Liu, Xin Gao, Levan Darjania, Jeffrey H. Chen, Francis Burrows, Ke Yu, Dana D. Hu-Lowe, Rasmus Hansen
Publikováno v:
Cancer Research. 77:5168-5168
The RAS/RAF/MEK pathway is a major driver of malignant progression, particularly in cancers arising from mutations in RAS, BRAF and NF1. Although both BRAF and MEK inhibitors have been approved for treatment of melanoma, their clinical activity is co
Autor:
Jingchuan Zhang, Patrick P. Zarrinkar, Ulf Peters, Levan Darjania, Shisheng Li, Rasmus Hansen, Ke Yu, Ata Zarieh, Shuangwei Li, Dana D. Hu-Lowe, Jolanta Grembecka, Pingda Ren, Linda Kessler, Szymon Klossowski, Duxin Sun, Francis Burrows, Yvonne Yao, Tess Ely, Lian-Sheng Li, Yi Liu, Yuan Liu, Katarzyna Kempińska, Hongzhi Miao, Jeff Kucharski, Tao Wu, Trupta Purohit, Bo Wen, Tomasz Cierpicki, Jun Feng, Brian M. Linhares, Yi Wang
Publikováno v:
Cancer Research. 77:5077-5077
Patients with MLL-rearranged leukemia typically have a poor prognosis. With chemotherapy and stem cell transplantation as current standard of care, the 5-year survival rate is estimated to be only about 35%. As the leukemogenic activity of MLL fusion
Autor:
Fabrice Pierre, Adam Siddiqui-Jain, Jeffrey P. Whitten, Ryan Stansfield, Levan Darjania, Cosmin Borsan, Sean O'Brien, Tran Joe, Chris Proffitt, May Omori, William G. Rice, Mustapha Haddach, Kenna Anderes, Nicholas B. Raffaele, Michael K. Schwaebe, Joshua R. Bliesath, Nicole Streiner, Suchitra Ravula, Diwata Macalino, Denis Drygin, Jerome Michaux, David M. Ryckman
Publikováno v:
ACS medicinal chemistry letters. 3(2)
Structure–activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. Compound 13 exhibited in v
Autor:
Jeffrey P. Whitten, Katy Trent, Caroline B. Ho, Kenna Anderes, Anne Vialettes, May Omori, Adam Siddiqui-Jain, Sean O'Brien, Johnny Y. Nagasawa, Michael K. Schwaebe, Eric Stefan, William G. Rice, Pauline Bourbon, Peter C. Chua, Ta Kung Chen, Chris Proffitt, Fabrice Pierre, Denis Drygin, Mustapha Haddach, Jerome Michaux, Nicole Streiner, Levan Darjania, David M. Ryckman, Ryan Stansfield, Josh Bliesath
Publikováno v:
Journal of medicinal chemistry. 54(2)
Herein we chronicle the discovery of CX-4945 (25n), a first-in-class, orally bioavailable ATP-competitive inhibitor of protein kinase CK2 in clinical trials for cancer. CK2 has long been considered a prime cancer drug target because of the roles of d
Autor:
Mustapha Haddach, Nicole Streiner, Caroline B. Ho, David M. Ryckman, Eric Stefan, William G. Rice, Fabrice Pierre, Kenna Anderes, Adam Siddiqui-Jain, Levan Darjania, Michael K. Schwaebe, Sean O'Brien, Pauline Bourbon, Ryan Stansfield
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
We describe the discovery of novel potent substituted pyrimido[4,5-c]quinoline ATP-competitive inhibitors of protein kinase CK2. A binding model of the inhibitors with the protein was elaborated on the basis of SAR and revealed various modes of inter
Autor:
N. Ichise, Hidetoshi Okuyama, Guy A. Thompson, Satoko Ichikawa, Takashi Okamoto, Levan Darjania
Publikováno v:
Biochemical Society Transactions. 28:725-727
Although glycosylphosphatidylinositol (GPI)-anchored proteins have now been found in several plants, very little is known regarding their metabolism there. This report describes studies of the biosynthesis and turnover of arabinogalactan proteins, a