New Perspectives, Opportunities, and Challenges in Exploring the Human Protein Kinome.
作者： Leah J. Wilson , Adam Linley , Dean E. Hammond , Fiona E. Hood , Judy M. Coulson
DOI: 10.1158/0008-5472.CAN-17-2291
关键词:
摘要: The human protein kinome comprises 535 proteins that, with the exception of approximately 50 pseudokinases, control intracellular signaling networks by catalyzing phosphorylation multiple substrates. While a major research focus last 30 years has been cancer-associated Tyr and Ser/Thr kinases, over 85% identified to be dysregulated in at least one disease or developmental disorder. Despite this remarkable statistic, for majority kinases there are currently no inhibitors progressing toward clinic, most cases, details their physiologic pathologic mechanisms remain partially obscure. By curating annotating data from literature public databases sites, associations, we generate an unbiased resource that highlights areas unmet need within kinome. We discuss strategies challenges associated characterizing catalytic noncatalytic outputs cells, describe successes new frontiers will support more comprehensive cancer-targeting therapeutic evaluation future. Cancer Res; 78(1); 15–29. ©2017 AACR.
aacrjournals.org
sci-hub.se 参考文章(172)
Matthew J Cooper, Nathan J Cox, Eric I Zimmerman, Brian J Dewar, James S Duncan, Martin C Whittle, Thien A Nguyen, Lauren S Jones, Sreerupa Ghose Roy, David M Smalley, Pei Fen Kuan, Kristy L Richards, Richard I Christopherson, Jian Jin, Stephen V Frye, Gary L Johnson, Albert S Baldwin, Lee M Graves, None, Application of Multiplexed Kinase Inhibitor Beads to Study Kinome Adaptations in Drug-Resistant Leukemia PLOS ONE. ,vol. 8, ,(2013) , 10.1371/JOURNAL.PONE.0066755
J. A. Engelman, K. Zejnullahu, T. Mitsudomi, Y. Song, C. Hyland, J. O. Park, N. Lindeman, C.-M. Gale, X. Zhao, J. Christensen, T. Kosaka, A. J. Holmes, A. M. Rogers, F. Cappuzzo, T. Mok, C. Lee, B. E. Johnson, L. C. Cantley, P. A. Janne, MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling Science. ,vol. 316, pp. 1039- 1043 ,(2007) , 10.1126/SCIENCE.1141478
Mercedes E Gorre, Mansoor Mohammed, Katharine Ellwood, Nicholas Hsu, Ron Paquette, P Nagesh Rao, Charles L Sawyers, Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification Science. ,vol. 293, pp. 876- 880 ,(2001) , 10.1126/SCIENCE.1062538
William Pao, Vincent A Miller, Katerina A Politi, Gregory J Riely, Romel Somwar, Maureen F Zakowski, Mark G Kris, Harold Varmus, Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain PLoS Medicine. ,vol. 2, pp. e73- ,(2005) , 10.1371/JOURNAL.PMED.0020073
Poulikos I. Poulikakos, Chao Zhang, Gideon Bollag, Kevan M. Shokat, Neal Rosen, RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF Nature. ,vol. 464, pp. 427- 430 ,(2010) , 10.1038/NATURE08902
Alberto Bardelli, Simona Corso, Andrea Bertotti, Sebastijan Hobor, Emanuele Valtorta, Giulia Siravegna, Andrea Sartore-Bianchi, Elisa Scala, Andrea Cassingena, Davide Zecchin, Maria Apicella, Giorgia Migliardi, Francesco Galimi, Calogero Lauricella, Carlo Zanon, Timothy Perera, Silvio Veronese, Giorgio Corti, Alessio Amatu, Marcello Gambacorta, Luis A. Diaz, Mark Sausen, Victor E. Velculescu, Paolo Comoglio, Livio Trusolino, Federica Di Nicolantonio, Silvia Giordano, Salvatore Siena, Amplification of the MET Receptor Drives Resistance to Anti-EGFR Therapies in Colorectal Cancer Cancer Discovery. ,vol. 3, pp. 658- 673 ,(2013) , 10.1158/2159-8290.CD-12-0558
C. M. Emery, K. G. Vijayendran, M. C. Zipser, A. M. Sawyer, L. Niu, J. J. Kim, C. Hatton, R. Chopra, P. A. Oberholzer, M. B. Karpova, L. E. MacConaill, J. Zhang, N. S. Gray, W. R. Sellers, R. Dummer, L. A. Garraway, MEK1 mutations confer resistance to MEK and B-RAF inhibition Proceedings of the National Academy of Sciences of the United States of America. ,vol. 106, pp. 20411- 20416 ,(2009) , 10.1073/PNAS.0905833106
Michael S Lawrence, Petar Stojanov, Paz Polak, Gregory V Kryukov, Kristian Cibulskis, Andrey Sivachenko, Scott L Carter, Chip Stewart, Craig H Mermel, Steven A Roberts, Adam Kiezun, Peter S Hammerman, Aaron McKenna, Yotam Drier, Lihua Zou, Alex H Ramos, Trevor J Pugh, Nicolas Stransky, Elena Helman, Jaegil Kim, Carrie Sougnez, Lauren Ambrogio, Elizabeth Nickerson, Erica Shefler, Maria L Cortés, Daniel Auclair, Gordon Saksena, Douglas Voet, Michael Noble, Daniel DiCara, Pei Lin, Lee Lichtenstein, David I Heiman, Timothy Fennell, Marcin Imielinski, Bryan Hernandez, Eran Hodis, Sylvan Baca, Austin M Dulak, Jens Lohr, Dan-Avi Landau, Catherine J Wu, Jorge Melendez-Zajgla, Alfredo Hidalgo-Miranda, Amnon Koren, Steven A McCarroll, Jaume Mora, Ryan S Lee, Brian Crompton, Robert Onofrio, Melissa Parkin, Wendy Winckler, Kristin Ardlie, Stacey B Gabriel, Charles WM Roberts, Jaclyn A Biegel, Kimberly Stegmaier, Adam J Bass, Levi A Garraway, Matthew Meyerson, Todd R Golub, Dmitry A Gordenin, Shamil Sunyaev, Eric S Lander, Gad Getz, None, Mutational heterogeneity in cancer and the search for new cancer-associated genes Nature. ,vol. 499, pp. 214- 218 ,(2013) , 10.1038/NATURE12213
Richard Bayliss, Andrew Fry, Tamanna Haq, Sharon Yeoh, On the molecular mechanisms of mitotic kinase activation Open Biology. ,vol. 2, pp. 120136- 120136 ,(2012) , 10.1098/RSOB.120136
Timothy J. Stuhlmiller, Samantha M. Miller, Jon S. Zawistowski, Kazuhiro Nakamura, Adriana S. Beltran, James S. Duncan, Steven P. Angus, Kyla A.L. Collins, Deborah A. Granger, Rachel A. Reuther, Lee M. Graves, Shawn M. Gomez, Pei-Fen Kuan, Joel S. Parker, Xin Chen, Noah Sciaky, Lisa A. Carey, H. Shelton Earp, Jian Jin, Gary L. Johnson, Inhibition of Lapatinib-Induced Kinome Reprogramming in ERBB2-Positive Breast Cancer by Targeting BET Family Bromodomains Cell Reports. ,vol. 11, pp. 390- 404 ,(2015) , 10.1016/J.CELREP.2015.03.037