14. Muller S et al (2015) The ins and outs of selective kinase inhibitor development. Nat Chem
Biol 11(11):818–821
15. Zheng J et al (1993) 2.2 a refined crystal structure of the catalytic subunit of cAMP-dependent
protein kinase complexed with MnATP and a peptide inhibitor. Acta Crystallogr D Biol
Crystallogr 49(Pt 3):362–365
16. Knighton DR et al (1991) Crystal structure of the catalytic subunit of cyclic adenosine
monophosphate-dependent protein kinase. Science 253(5018):407–414
17. Taylor SS et al (1992) Structural framework for the protein kinase family. Annu Rev Cell Biol
8:429–462
18. Fabbro D, Cowan-Jacob SW, Moebitz H (2015) Ten things you should know about protein
kinases: IUPHAR review 14. Br J Pharmacol 172(11):2675–2700
19. Nolen B, Taylor S, Ghosh G (2004) Regulation of protein kinases; controlling activity through
activation segment conformation. Mol Cell 15(5):661–675
20. Adams JA (2003) Activation loop phosphorylation and catalysis in protein kinases: is there
functional evidence for the autoinhibitor model? Biochemistry 42(3):601–607
21. Johnson LN, Lewis RJ (2001) Structural basis for control by phosphorylation. Chem Rev
101(8):2209–2242
22. Roskoski Jr R (2015) A historical overview of protein kinases and their targeted small
molecule inhibitors. Pharmacol Res 100:1–23
23. Kornev AP et al (2006) Surface comparison of active and inactive protein kinases identifies
a conserved activation mechanism. Proc Natl Acad Sci U S A 103(47):17783–17788
24. Kornev AP, Taylor SS (2015) Dynamics-driven allostery in protein kinases. Trends Biochem
Sci 40(11):628–647
25. Ten Eyck LF, Taylor SS, Kornev AP (2008) Conserved spatial patterns across the protein
kinase family. Biochim Biophys Acta 1784(1):238–243
26. Taylor SS, Kornev AP (2011) Protein kinases: evolution of dynamic regulatory proteins.
Trends Biochem Sci 36(2):65–77
27. Yang J et al (2009) Contribution of non-catalytic core residues to activity and regulation
in protein kinase A. J Biol Chem 284(10):6241–6248
28. Bishop AC et al (2000) A chemical switch for inhibitor-sensitive alleles of any protein kinase.
Nature 407(6802):395–401
29. Yun CH et al (2008) The T790M mutation in EGFR kinase causes drug resistance by
increasing the affinity for ATP. Proc Natl Acad Sci U S A 105(6):2070–2075
30. Azam M et al (2008) Activation of tyrosine kinases by mutation of the gatekeeper threonine.
Nat Struct Mol Biol 15(10):1109–1118
31. Sicheri F, Moarefi I, Kuriyan J (1997) Crystal structure of the Src family tyrosine kinase Hck.
Nature 385(6617):602–609
32. Meng W et al (2002) Structure of mitogen-activated protein kinase-activated protein
(MAPKAP) kinase 2 suggests a bifunctional switch that couples kinase activation with nuclear
export. J Biol Chem 277(40):37401–37405
33. Prowse CN, Lew J (2001) Mechanism of activation of ERK2 by dual phosphorylation.
J Biol Chem 276(1):99–103
34. Dajani R et al (2003) Structural basis for recruitment of glycogen synthase kinase 3beta to
the axin-APC scaffold complex. EMBO J 22(3):494–501
35. Weiss A, Schlessinger J (1998) Switching signals on or off by receptor dimerization. Cell
94(3):277–280
36. Mellado M et al (2001) Chemokine signaling and functional responses: the role of receptor
dimerization and TK pathway activation. Annu Rev Immunol 19:397–421
37. Rellos P et al (2010) Structure of the CaMKIIdelta/calmodulin complex reveals the molecular
mechanism of CaMKII kinase activation. PLoS Biol 8(7):e1000426
38. Rosenberg OS et al (2006) Oligomerization states of the association domain and the
holoenyzme of Ca2+/CaM kinase II. FEBS J 273(4):682–694
39. Rosenberg OS et al (2005) Structure of the autoinhibited kinase domain of CaMKII and SAXS
analysis of the holoenzyme. Cell 123(5):849–860
Function, Structure and Topology of Protein Kinases
19
Biol 11(11):818–821
15. Zheng J et al (1993) 2.2 a refined crystal structure of the catalytic subunit of cAMP-dependent
protein kinase complexed with MnATP and a peptide inhibitor. Acta Crystallogr D Biol
Crystallogr 49(Pt 3):362–365
16. Knighton DR et al (1991) Crystal structure of the catalytic subunit of cyclic adenosine
monophosphate-dependent protein kinase. Science 253(5018):407–414
17. Taylor SS et al (1992) Structural framework for the protein kinase family. Annu Rev Cell Biol
8:429–462
18. Fabbro D, Cowan-Jacob SW, Moebitz H (2015) Ten things you should know about protein
kinases: IUPHAR review 14. Br J Pharmacol 172(11):2675–2700
19. Nolen B, Taylor S, Ghosh G (2004) Regulation of protein kinases; controlling activity through
activation segment conformation. Mol Cell 15(5):661–675
20. Adams JA (2003) Activation loop phosphorylation and catalysis in protein kinases: is there
functional evidence for the autoinhibitor model? Biochemistry 42(3):601–607
21. Johnson LN, Lewis RJ (2001) Structural basis for control by phosphorylation. Chem Rev
101(8):2209–2242
22. Roskoski Jr R (2015) A historical overview of protein kinases and their targeted small
molecule inhibitors. Pharmacol Res 100:1–23
23. Kornev AP et al (2006) Surface comparison of active and inactive protein kinases identifies
a conserved activation mechanism. Proc Natl Acad Sci U S A 103(47):17783–17788
24. Kornev AP, Taylor SS (2015) Dynamics-driven allostery in protein kinases. Trends Biochem
Sci 40(11):628–647
25. Ten Eyck LF, Taylor SS, Kornev AP (2008) Conserved spatial patterns across the protein
kinase family. Biochim Biophys Acta 1784(1):238–243
26. Taylor SS, Kornev AP (2011) Protein kinases: evolution of dynamic regulatory proteins.
Trends Biochem Sci 36(2):65–77
27. Yang J et al (2009) Contribution of non-catalytic core residues to activity and regulation
in protein kinase A. J Biol Chem 284(10):6241–6248
28. Bishop AC et al (2000) A chemical switch for inhibitor-sensitive alleles of any protein kinase.
Nature 407(6802):395–401
29. Yun CH et al (2008) The T790M mutation in EGFR kinase causes drug resistance by
increasing the affinity for ATP. Proc Natl Acad Sci U S A 105(6):2070–2075
30. Azam M et al (2008) Activation of tyrosine kinases by mutation of the gatekeeper threonine.
Nat Struct Mol Biol 15(10):1109–1118
31. Sicheri F, Moarefi I, Kuriyan J (1997) Crystal structure of the Src family tyrosine kinase Hck.
Nature 385(6617):602–609
32. Meng W et al (2002) Structure of mitogen-activated protein kinase-activated protein
(MAPKAP) kinase 2 suggests a bifunctional switch that couples kinase activation with nuclear
export. J Biol Chem 277(40):37401–37405
33. Prowse CN, Lew J (2001) Mechanism of activation of ERK2 by dual phosphorylation.
J Biol Chem 276(1):99–103
34. Dajani R et al (2003) Structural basis for recruitment of glycogen synthase kinase 3beta to
the axin-APC scaffold complex. EMBO J 22(3):494–501
35. Weiss A, Schlessinger J (1998) Switching signals on or off by receptor dimerization. Cell
94(3):277–280
36. Mellado M et al (2001) Chemokine signaling and functional responses: the role of receptor
dimerization and TK pathway activation. Annu Rev Immunol 19:397–421
37. Rellos P et al (2010) Structure of the CaMKIIdelta/calmodulin complex reveals the molecular
mechanism of CaMKII kinase activation. PLoS Biol 8(7):e1000426
38. Rosenberg OS et al (2006) Oligomerization states of the association domain and the
holoenyzme of Ca2+/CaM kinase II. FEBS J 273(4):682–694
39. Rosenberg OS et al (2005) Structure of the autoinhibited kinase domain of CaMKII and SAXS
analysis of the holoenzyme. Cell 123(5):849–860
Function, Structure and Topology of Protein Kinases
19