By Peter Simunovich, John-Paul Brisigotti, Mike Haught
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Extra info for Burning Empires (Battlefront Minatures)
This region can be found between the APE motif and the C-terminus and is typical for all CMGC kinases. It is also called the “CDK insert” region as Cak binds here for T-loop activation by phosphorylation [41, 149] CK1 The protein kinase CK1 (formerly called Casein Kinase 1) group represents a typically small but essential group of EPKs found in all eukaryotes CK1, Tau tubulin kinase RGC The members of the small group of receptor guanylate cyclases (RGCs) are similar in sequence to the metazoan Tyr kinases which are lacking in plants, fungi, and protists.
The activation segment of kinases is also known to literally form “assembly platforms” whereby catalytic residues of the kinase and substrate phosphoacceptors can approach in the closest proximity for a successful nucleophilic phosphoryl transfer (40, 46). With some of the early crystal structures of human EPKs, such as for Cdk2 and MAPK, it was shown that the activation loop reduces access to the substrate site (Cdk2 (57) and MAPK (58)). g. PKA (protein kinase A/cAMPdependent PK/cAPK), a different role was proposed.
J Med Chem 50, 409–24. 38. , and Gray, N. S. (2006) Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol 2, 358–64. 39. Johnson, L. N. (2009) The regulation of protein phosphorylation. Biochem Soc Trans 37, 627–41. 40. , and Kuriyan, J. (2002) The conformational plasticity of protein kinases. Cell 109, 275–82. 41. , and Ghosh, G. (2004) Regulation of protein kinases; controlling activity through activation segment conformation. Mol Cell 15, 661–75. 42. , and Neuwald, A.