STK33 kinase inhibitor BRD-8899 has no effect on KRAS-dependent cancer cell viability

作者: T. Luo , K. Masson , J. D. Jaffe , W. Silkworth , N. T. Ross

DOI: 10.1073/PNAS.1120589109

关键词:

摘要: … STK33 might have therapeutic benefit in these cancers. Here, we describe the development of selective, low nanomolar inhibitors of STK33’… view that inhibition of STK33’s kinase activity …

参考文章(24)
Christine Breitenlechner, Michael Gaßel, Hiroyoshi Hidaka, Volker Kinzel, Robert Huber, Richard A Engh, Dirk Bossemeyer, Protein Kinase A in Complex with Rho-Kinase Inhibitors Y-27632, Fasudil, and H-1152P: Structural Basis of Selectivity Structure. ,vol. 11, pp. 1595- 1607 ,(2003) , 10.1016/J.STR.2003.11.002
Henrik Daub, Jesper V Olsen, Michaela Bairlein, Florian Gnad, Felix S Oppermann, Roman Körner, Zoltán Greff, György Kéri, Olaf Stemmann, Matthias Mann, None, Kinase-Selective Enrichment Enables Quantitative Phosphoproteomics of the Kinome across the Cell Cycle Molecular Cell. ,vol. 31, pp. 438- 448 ,(2008) , 10.1016/J.MOLCEL.2008.07.007
Carol Babij, Yihong Zhang, Robert J. Kurzeja, Anke Munzli, Amro Shehabeldin, Manory Fernando, Kim Quon, Paul D. Kassner, Astrid A. Ruefli-Brasse, Vivienne J. Watson, Flordeliza Fajardo, Angela Jackson, James Zondlo, Yu Sun, Aaron R. Ellison, Cherylene A. Plewa, Miguel Tisha San, John Robinson, John McCarter, Ralf Schwandner, Ted Judd, Josette Carnahan, Isabelle Dussault, STK33 Kinase Activity Is Nonessential in KRAS-Dependent Cancer Cells Cancer Research. ,vol. 71, pp. 5818- 5826 ,(2011) , 10.1158/0008-5472.CAN-11-0778
Ji-Hu Zhang, Thomas D. Y. Chung, Kevin R. Oldenburg, A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. Journal of Biomolecular Screening. ,vol. 4, pp. 67- 73 ,(1999) , 10.1177/108705719900400206
Bret B. Friday, Alex A. Adjei, K-ras as a target for cancer therapy. Biochimica et Biophysica Acta. ,vol. 1756, pp. 127- 144 ,(2005) , 10.1016/J.BBCAN.2005.08.001
Jeffrey A Engelman, Liang Chen, Xiaohong Tan, Katherine Crosby, Alexander R Guimaraes, Rabi Upadhyay, Michel Maira, Kate McNamara, Samanthi A Perera, Youngchul Song, Lucian R Chirieac, Ramneet Kaur, Angela Lightbown, Jessica Simendinger, Timothy Li, Robert F Padera, Carlos García-Echeverría, Ralph Weissleder, Umar Mahmood, Lewis C Cantley, Kwok-Kin Wong, Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers Nature Medicine. ,vol. 14, pp. 1351- 1356 ,(2008) , 10.1038/NM.1890
Antoine E. Karnoub, Robert A. Weinberg, Ras oncogenes: split personalities Nature Reviews Molecular Cell Biology. ,vol. 9, pp. 517- 531 ,(2008) , 10.1038/NRM2438
Ji Luo, Michael J. Emanuele, Danan Li, Chad J. Creighton, Michael R. Schlabach, Thomas F. Westbrook, Kwok-Kin Wong, Stephen J. Elledge, A Genome-wide RNAi Screen Identifies Multiple Synthetic Lethal Interactions with the Ras Oncogene Cell. ,vol. 137, pp. 835- 848 ,(2009) , 10.1016/J.CELL.2009.05.006
John T. Prince, Natalie G. Ahn, The Case of the Disappearing Drug Target Molecular Cell. ,vol. 37, pp. 455- 456 ,(2010) , 10.1016/J.MOLCEL.2010.02.010