26. Jacobs MD, Caron PR, Hare BJ (2008) Classifying protein kinase structures guides use of
ligand-selectivity profiles to predict inactive conformations: structure of lck/imatinib complex.
Proteins 70:1451–1460
27. Zarrinkar PP et al (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotech
29:1046–1051
28. Fabbro D, Cowan-Jacob SW, Moebitz H (2015) Ten things you should know about protein
kinases. Br J Pharmacol 172:2675–2700
29. Palmieri L, Rastelli G (2013) αC helix displacement as a general approach for allosteric
modulation of protein kinases. Drug Discov Today 18:407–414
30. Gilmer TM (2008) Impact of common epidermal growth factor receptor and HER2 variants on
receptor activity and inhibition by Lapatinib. Cancer Res 68:571–579
31. Hochegger H, Hegarat N, Pereira-Leal JB (2013) Aurora at the pole and equator: overlapping
functions of Aurora kinases in the mitotic spindle. Open Biol. https://doi.org/10.1098/rsob.
120185
32. Saya H (2002) Roles of aurora A kinase in mitotic entry and G2 checkpoint in mammalian cells.
Genes Cells 7:1173–1182
33. Lampson MA, Cheeseman IM (2011) Sensing centromere tension: aurora B and the regulation
of kinetochore function. Trends Cell Biol 21:133–140
34. Quartuccio SM, Schindler K (2015) Functions of Aurora kinase C in meiosis and cancer. Front
Cell Dev Biol. https://doi.org/10.3389/fcell.2015.00050
35. Katayama H, Brinkley WR, Sen S (2003) The Aurora kinases: role in cell transformation and
tumorigenesis. Cancer Metastasis Rev 22:451–464
36. Goldenson B, Crispino JD (2015) The aurora kinases in cell cycle and leukemia. Oncogene
34:537–545
37. Tang A, Gao K, Chu L, Zhang R, Yang J, Zheng J (2017) Aurora kinases: novel therapy targets
in cancers. Oncotarget 8(14):23937–23954
38. Keen N, Taylor S (2004) Aurora-kinase inhibitors as anticancer agents. Nat Rev Cancer
4:927–936
39. Carry JC, Clerc F, Minoux H et al (2015) SAR156497, an exquisitely selective inhibitor of
aurora kinases. J Med Chem 58:362–375
40. Roskoski R (2016) Classification of small molecule protein kinase inhibitors based upon the
structures of their drug-enzyme complexes. Pharmacol Res 103:26–48
41. Tong M, Seeliger MA (2015) Targeting conformational plasticity of protein kinases. ACS
Chem Biol 10:190–200
42. Organ SL, Tsao MS (2011) An overview of the c-MET signaling pathway. Ther Adv Med
Oncol 3(1 Suppl):S7–S19
43. Zhang J, Babic A (2016) Regulation of the MET oncogene: molecular mechanisms. Carcinogenesis 37:345–355
44. Tovar EA, Graveel CR (2017) MET in human cancer: germline and somatic mutations. Ann
Trans Med 5(10):205. https://doi.org/10.21037/atm.2017.03.64
45. Dixit A, Torkamani A, Schork NJ, Verkhivker G (2009) Computational modeling of structurally conserved cancer mutations in the RET and MET kinases: the impact on protein structure,
dynamics, and stability. Biophys J 96:858–874
46. Xu J, Wang J, Zhang S (2017) Mechanisms of resistance to irreversible epidermal growth factor
receptor tyrosine kinase inhibitors and therapeutic strategies in non-small cell lung cancer.
Oncotarget 8(52):90557–90578
47. Soria JC et al (2012) ALK translocation and crizotinib in non-small cell lung cancer: an evolving
paradigm in oncology drug development. Eur J Cancer 48:961–973
48. Mo HN, Liu P (2017) Targeting MET in cancer therapy. Chronic Dis Trans Med 3(3):148–153
49. Schio L, Nemecek C, Ugolini T et al (2012) SAR125844: a potent and selective
ATP-competitive inhibitor of MET kinase. Cancer Res 72(8, Suppl.1):2911
50. Schio L et al (2016) Discovery, pharmacokinetic and pharmacological properties of the potent
and selective MET kinase inhibitor, 1-{6-[6-(4-Fluoro-phenyl)-[1,2,4]triazolo[4,3-b]pyridazinAchieving High Levels of Selectivity for Kinase Inhibitors
121
ligand-selectivity profiles to predict inactive conformations: structure of lck/imatinib complex.
Proteins 70:1451–1460
27. Zarrinkar PP et al (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotech
29:1046–1051
28. Fabbro D, Cowan-Jacob SW, Moebitz H (2015) Ten things you should know about protein
kinases. Br J Pharmacol 172:2675–2700
29. Palmieri L, Rastelli G (2013) αC helix displacement as a general approach for allosteric
modulation of protein kinases. Drug Discov Today 18:407–414
30. Gilmer TM (2008) Impact of common epidermal growth factor receptor and HER2 variants on
receptor activity and inhibition by Lapatinib. Cancer Res 68:571–579
31. Hochegger H, Hegarat N, Pereira-Leal JB (2013) Aurora at the pole and equator: overlapping
functions of Aurora kinases in the mitotic spindle. Open Biol. https://doi.org/10.1098/rsob.
120185
32. Saya H (2002) Roles of aurora A kinase in mitotic entry and G2 checkpoint in mammalian cells.
Genes Cells 7:1173–1182
33. Lampson MA, Cheeseman IM (2011) Sensing centromere tension: aurora B and the regulation
of kinetochore function. Trends Cell Biol 21:133–140
34. Quartuccio SM, Schindler K (2015) Functions of Aurora kinase C in meiosis and cancer. Front
Cell Dev Biol. https://doi.org/10.3389/fcell.2015.00050
35. Katayama H, Brinkley WR, Sen S (2003) The Aurora kinases: role in cell transformation and
tumorigenesis. Cancer Metastasis Rev 22:451–464
36. Goldenson B, Crispino JD (2015) The aurora kinases in cell cycle and leukemia. Oncogene
34:537–545
37. Tang A, Gao K, Chu L, Zhang R, Yang J, Zheng J (2017) Aurora kinases: novel therapy targets
in cancers. Oncotarget 8(14):23937–23954
38. Keen N, Taylor S (2004) Aurora-kinase inhibitors as anticancer agents. Nat Rev Cancer
4:927–936
39. Carry JC, Clerc F, Minoux H et al (2015) SAR156497, an exquisitely selective inhibitor of
aurora kinases. J Med Chem 58:362–375
40. Roskoski R (2016) Classification of small molecule protein kinase inhibitors based upon the
structures of their drug-enzyme complexes. Pharmacol Res 103:26–48
41. Tong M, Seeliger MA (2015) Targeting conformational plasticity of protein kinases. ACS
Chem Biol 10:190–200
42. Organ SL, Tsao MS (2011) An overview of the c-MET signaling pathway. Ther Adv Med
Oncol 3(1 Suppl):S7–S19
43. Zhang J, Babic A (2016) Regulation of the MET oncogene: molecular mechanisms. Carcinogenesis 37:345–355
44. Tovar EA, Graveel CR (2017) MET in human cancer: germline and somatic mutations. Ann
Trans Med 5(10):205. https://doi.org/10.21037/atm.2017.03.64
45. Dixit A, Torkamani A, Schork NJ, Verkhivker G (2009) Computational modeling of structurally conserved cancer mutations in the RET and MET kinases: the impact on protein structure,
dynamics, and stability. Biophys J 96:858–874
46. Xu J, Wang J, Zhang S (2017) Mechanisms of resistance to irreversible epidermal growth factor
receptor tyrosine kinase inhibitors and therapeutic strategies in non-small cell lung cancer.
Oncotarget 8(52):90557–90578
47. Soria JC et al (2012) ALK translocation and crizotinib in non-small cell lung cancer: an evolving
paradigm in oncology drug development. Eur J Cancer 48:961–973
48. Mo HN, Liu P (2017) Targeting MET in cancer therapy. Chronic Dis Trans Med 3(3):148–153
49. Schio L, Nemecek C, Ugolini T et al (2012) SAR125844: a potent and selective
ATP-competitive inhibitor of MET kinase. Cancer Res 72(8, Suppl.1):2911
50. Schio L et al (2016) Discovery, pharmacokinetic and pharmacological properties of the potent
and selective MET kinase inhibitor, 1-{6-[6-(4-Fluoro-phenyl)-[1,2,4]triazolo[4,3-b]pyridazinAchieving High Levels of Selectivity for Kinase Inhibitors
121