1. Schiffer, C. A. BCR–ABL tyrosine kinase inhibitors for chronic myelogenous leukemia. N. Engl. J. Med. 357, 258–265 (2007).
2. Baselga, J. Targeting tyrosine kinases in cancer: the second wave. Science 312, 1175–1178 (2006).
3. Collins, I. & Workman, P. New approaches to molecular cancer therapeutics. Nature Chem. Biol. 2, 689–700 (2006).
4. Sebolt-Leopold, J. S. & English, J. M. Mechanisms of drug inhibition of signalling molecules. Nature 441, 457–462 (2006).
5. Verweij, J. & de Jonge, M. Multitarget tyrosine kinase inhibition: [and the winner is...]. J. Clin. Oncol. 25, 2340–2342 (2007).
6. Boehm, J. S. et al. Integrative genomic approaches identify IKBKE as a breast cancer oncogene. Cell 129, 1065–1079 (2007).
7. Buckbinder, L. et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc. Natl Acad. Sci. USA 104, 10619–10624 (2007).
8. Carpten, J. D. et al. A transforming mutation in the pleckstrin homology domain of AKT1 in cancer. Nature 448, 439–444 (2007).
9. Davies, H. et al. Mutations of the BRAF gene in human cancer. Nature 417, 949–954 (2002).
10. Engelman, J. A. et al. MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science 316, 1039–1043 (2007).
11. Mahajan, N. P. et al. Activated Cdc42-associated kinase Ack1 promotes prostate cancer progression via androgen receptor tyrosine phosphorylation. Proc. Natl Acad. Sci. USA 104, 8438–8443 (2007).
12. Ruckle, T., Schwarz, M. K. & Rommel, C. PI3Kγ inhibition: towards an 'aspirin of the 21st century'? Nature Rev. Drug Discov. 5, 903–918 (2006).
13. Smith, W. W. et al. Kinase activity of mutant LRRK2 mediates neuronal toxicity. Nature Neurosci. 9, 1231–1233 (2006).
14. Soda, M. et al. Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer. Nature 448, 561–566 (2007).
15. Strebhardt, K. & Ullrich, A. Targeting polo-like kinase 1 for cancer therapy. Nature Rev. Cancer 6, 321–330 (2006).
16. Tefferi, A. JAK2 mutations in polycythemia vera — molecular mechanisms and clinical applications. N. Engl. J. Med. 356, 444–445 (2007).
17. Tse, A. N., Carvajal, R. & Schwartz, G. K. Targeting checkpoint kinase 1 in cancer therapeutics. Clin. Cancer Res. 13, 1955–1960 (2007).
18. Hayashi, M. L. et al. Inhibition of p21-activated kinase rescues symptoms of fragile X syndrome in mice. Proc. Natl Acad. Sci. USA 104, 11489–11494 (2007).
19. Whartenby, K. A. et al. Inhibition of FLT3 signaling targets DCs to ameliorate autoimmune disease. Proc. Natl Acad. Sci. USA 102, 16741–16746 (2005).
20. Changelian, P. S. et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science 302, 875–878 (2003).
21. Solinas, G. et al. JNK1 in hematopoietically derived cells contributes to diet-induced inflammation and insulin resistance without affecting obesity. Cell Metab. 6, 386–397 (2007).
22. Morwick, T. et al. Evolution of the thienopyridine class of inhibitors of IκB kinase-β: part I: hit-to-lead strategies. J. Med. Chem. 49, 2898–2908 (2006).
23. Pevarello, P. et al. 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. J. Med. Chem. 47, 3367–3380 (2004).
24. Wittman, M. et al. Discovery of a (1 H-benzoimidazol-2-yl)-1 H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J. Med. Chem. 48, 5639–5643 (2005).
25. Bach, S. et al. Roscovitine targets, protein kinases and pyridoxal kinase. J. Biol. Chem. 280, 31208–31219 (2005).
26. Bain, J. et al. The selectivity of protein kinase inhibitors: a further update. Biochem. J. 408, 297–315 (2007).
