Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2.

作者: Alison M. Lawrie , Martin E.M. Noble , Paul Tunnah , Nicholas R. Brown , Louise N. Johnson

DOI: 10.1038/NSB1097-796

关键词: Cell biologyProtein kinase ACyclin-dependent kinase 2StaurosporineCyclin-dependent kinaseKinaseBiologyMitogen-activated protein kinase kinaseProtein structurec-Raf

摘要: Staurosporine exhibits nanomolar IC50 values against a wide range of protein kinases. The structure CDK2 staurosporine complex explains the tight binding this inhibitor, and suggests features to be exploited in design specific inhibitors CDKs.

参考文章(37)
Geoffrey J. Barton, Protein multiple sequence alignment and flexible pattern matching. Methods in Enzymology. ,vol. 183, pp. 403- 428 ,(1990) , 10.1016/0076-6879(90)83027-7
Flavio Meggio, Arianna Donella Deana, Maria Ruzzene, Anna M. Brunati, Luca Cesaro, Barbara Guerra, Thomas Meyer, Helmut Mett, Doriano Fabbro, Pascal Furet, Grazyna Dobrowolska, Lorenzo A. Pinna, Different susceptibility of protein kinases to staurosporine inhibition Kinetic studies and molecular bases for the resistance of protein kinase CK2 FEBS Journal. ,vol. 234, pp. 317- 322 ,(1995) , 10.1111/J.1432-1033.1995.317_C.X
Tatsuya Tamaoki, Hisayo Nomoto, Isami Takahashi, Yuzuru Kato, Makoto Morimoto, Fusao Tomita, Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase. Biochemical and Biophysical Research Communications. ,vol. 135, pp. 397- 402 ,(1986) , 10.1016/0006-291X(86)90008-2
D. Toullec, P. Pianetti, H. Coste, P. Bellevergue, T. Grand-Perret, M. Ajakane, V. Baudet, P. Boissin, E. Boursier, F. Loriolle, The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. Journal of Biological Chemistry. ,vol. 266, pp. 15771- 15781 ,(1991) , 10.1016/S0021-9258(18)98476-0
Alicia A. Russo, Philip D. Jeffrey, Nikola P. Pavletich, Structural basis of cyclin-dependent kinase activation by phosphorylation. Nature Structural & Molecular Biology. ,vol. 3, pp. 696- 700 ,(1996) , 10.1038/NSB0896-696
Walter Filgueira de Azevedo Jr., S Leclerc, L Meijer, L Havlicek, M Strnad, SH Kim, Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine. FEBS Journal. ,vol. 243, pp. 518- 526 ,(1997) , 10.1111/J.1432-1033.1997.0518A.X
Uwe Trinks, Elisabeth Buchdunger, Pascal Furet, Wilhelm Kump, Helmut Mett, Thomas Meyer, Marcel Mueller, Urs Regenass, Greti Rihs, Dianilinophthalimides : potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase Journal of Medicinal Chemistry. ,vol. 37, pp. 1015- 1027 ,(1994) , 10.1021/JM00033A019
E. Buchdunger, U. Trinks, H. Mett, U. Regenass, M. Muller, T. Meyer, E. McGlynn, L. A. Pinna, P. Traxler, N. B. Lydon, 4,5-Dianilinophthalimide: a protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity Proceedings of the National Academy of Sciences of the United States of America. ,vol. 91, pp. 2334- 2338 ,(1994) , 10.1073/PNAS.91.6.2334