The protein kinase activity modulation sites: Mechanisms for cellular regulation - Targets for therapeutic intervention

Advances in Enzyme Regulation

Volumn 41, Issue 1, 2001, Pages 121-149

  Engh, Richard A ^a,b   Bossemeyer, Dirk ^c  

^a ROCHE DIAGNOSTICS GMBH   (Germany)

^b MAX PLANCK INSTITUTE OF BIOCHEMISTRY   (Germany)

^c GERMAN CANCER RESEARCH CENTER DKFZ   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATE; CALMODULIN; CONNECTIN; CYCLIC AMP DEPENDENT PROTEIN KINASE; CYCLIC AMP DEPENDENT PROTEIN KINASES; CYCLIN DEPENDENT KINASE; CYCLINE; ENZYME INHIBITOR; FIBROBLAST GROWTH FACTOR RECEPTOR; GLYCINE; GUANOSINE TRIPHOSPHATE; INSULIN RECEPTOR; ISOPROTEIN; LIGAND; MITOGEN ACTIVATED PROTEIN KINASE; PHOSPHORYLASE KINASE; PROTEIN KINASE; PROTEIN KINASE (CALCIUM,CALMODULIN); PROTEIN SERINE THREONINE KINASE; PROTEIN TYROSINE KINASE; SERINE; STAUROSPORINE; THREONINE; TRANSFORMING GROWTH FACTOR BETA RECEPTOR; TYROSINE;

ANIMAL; ARTICLE; BINDING SITE; BIOLOGICAL MODEL; CHEMICAL STRUCTURE; CRYSTAL STRUCTURE; ENZYME ACTIVE SITE; ENZYME ACTIVITY; HUMAN; HUMAN CELL; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN SECONDARY STRUCTURE; PROTEIN TERTIARY STRUCTURE; REGULATORY MECHANISM; SIGNAL TRANSDUCTION;

ANIMALIA; EUKARYOTA;

EID: 0034989316     PISSN: 00652571     EISSN: None     Source Type: Book Series    
DOI: 10.1016/S0065-2571(00)00010-8     Document Type: Article

References (75)

1. Cancer cell cycles
2. Frequent somatic mutations and homozygous deletions of the p16 (MTS1) gene in pancreatic adenocarcinoma
3. CDK inhibition and cancer therapy
4. The structure-based design of ATP-site directed protein kinase inhibitors
5. Structures of staurosporine bound to CDK2 and cAPK - New tools for structure-based design of protein kinase inhibitors
6. Inhibitors of p38 MAP kinase, therapeutic intervention in cytokine-mediated diseases
7. Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase
8. Crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MgATP and peptide inhibitor
9. Phosphotransferase and substrate binding mechanism of the cAMP-dependent protein kinase catalytic subunit from porcine heart as deduced from the 2.0 A structure of the complex with Mn2 + adenylyl imidodiphosphate and inhibitor peptide PKI(5-24)
10. Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase
11. The crystal structure of a phosphorylase kinase peptide substrate complex, kinase, substrate recognition
12. Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog
13. Protein modification, docking sites for kinases
14. Protein kinase catalytic domain sequence database, identification of conserved features of primary structure and classification of family members
15. Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity
16. The glycine-rich sequence of protein kinases, a multifunctional element
17. A binary complex of the catalytic subunit of cAMP-dependent protein kinase and adenosine further defines conformational flexibility
18. Crystal structures of the myristylated catalytic subunit of cAMP-dependent protein kinase reveal open and closed conformations
19. Active and inactive protein kinases, structural basis for regulation
20. In vivo activation of recombinant cAPK catalytic subunit active site mutants by coexpression of the wild-type enzyme, evidence for intermolecular cotranslational phosphorylation
21. Phosphorylation and activation of cAMP-dependent protein kinase by phosphoinositide-dependent protein kinase
22. Dephosphorylation of catalytic subunit of cAMP-dependent protein kinase at Thr-197 by a cellular protein phosphatase and by purified protein phosphatase-2A
23. Phosphorylation modulates catalytic function and regulation in the cAMP-dependent protein kinase
24. The Eleventh Datta Lecture. The structural basis for substrate recognition control by protein kinases
25. Crystal structure of the tyrosine kinase domain of the human insulin receptor
26. Crystal structure of cyclin-dependent kinase 2
27. Regulation of CDKs by phosphorylation
28. Effects of phosphorylation of threonine 160 on cyclin-dependent kinase 2 structure and activity
29. Mechanism of CDK activation revealed by the structure of a cyclinA-CDK2 complex
30. Mechanisms of cyclin-dependent kinase regulation, structures of Cdks, their cyclin activators, and Cip and INK4 inhibitors
31. The structural basis for specificity of substrate and recruitment peptides for cyclin-dependent kinases
32. Structural basis of cyclin-dependent kinase activation by phosphorylation
33. Kinetic analyses of mutations in the glycine-rich loop of cAMP-dependent protein kinase
34. Crystal structure of the p27Kip1 cyclin-dependent-kinase inhibitor bound to the cyclin A-Cdk2 complex
35. Structural basis for inhibition of the cyclin-dependent kinase Cdk6 by the tumour suppressor p16(INK4a)
36. Crystal structure of the complex of the cyclin D-dependent kinase Cdk6 bound to the cell-cycle inhibitor p19INK4d
37. Crystal structure and mutational analysis of the human CDK2 kinase complex with cell cycle-regulatory protein CksHs1
38. Cyclin-dependent kinase and Cks/Suc1 interact with the proteasome in yeast to control proteolysis of M-phase targets
39. Structure-function relationships in Src family and related protein tyrosine kinases
40. Crystal structures of c-Src reveal features of its autoinhibitory mechanism
41. Structural basis for activation of human lymphocyte kinase Lck upon tyrosine phosphorylation
42. The 2.35 A crystal structure of the inactivated form of chicken Src, a dynamic molecule with multiple regulatory interactions
43. Three-dimensional structure of the tyrosine kinase c-Src
44. Crystal structure of the Src family tyrosine kinase Hck
45. Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor
46. Transmembrane signaling by the human insulin receptor kinase. Relationship between intramolecular beta subunit trans-, cis-autophosphorylation and substrate kinase activation
47. Structure of the FGF receptor tyrosine kinase domain reveals a novel autoinhibitory mechanism
48. Autoregulatory mechanisms in protein-tyrosine kinases
49. Crystal structure of the cytoplasmic domain of the type I TGF beta receptor in complex with FKBP12
50. Structural basis for the autoinhibition of calcium/calmodulin-dependent protein kinase I
51. Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase
52. Insights into autoregulation from the crystal structure of twitchin kinase
53. Substrate and pseudosubstrate interactions with protein kinases determinants of specificity
54. Structural basis for activation of the titin kinase domain during myofibrillogenesis
55. Identification of the regulatory phosphorylation sites in pp42/mitogen-activated protein kinase (MAP kinase)
56. Crystal structure of p38 mitogen-activated protein kinase
57. The structure of phosphorylated p38gamma is monomeric and reveals a conserved activation-loop conformation
58. Atomic structure of the MAP kinase ERK2 at 2.3 A resolution
59. Activation mechanism of the MAP kinase ERK2 by dual phosphorylation
60. Crystal structure of JNK3, a kinase implicated in neuronal apoptosis
61. The structure of mitogen-activated protein kinase p38 at 2.1-A resolution
62. Three-dimensional structure of mammalian casein kinase I, molecular basis for phosphate recognition
63. Crystal structure of casein kinase-1, a phosphate-directed protein kinase
64. Human casein kinase II, structures, genes, expression and requirement in cell growth stimulation
65. Crystal structure of the catalytic subunit of protein kinase CK2 from Zea mays at 2.1 A resolution
66. GTP plus water mimic ATP in the active site of protein kinase CK2
67. Characterization of the regulatory domain of the gamma-subunit of phosphorylase kinase. The two noncontiguous calmodulin-binding subdomains are also autoinhibitory
68. Two structures of the catalytic domain of phosphorylase kinase, an active protein kinase complexed with substrate analogue and product
69. The crystal structure of the Physarum polycephalum actin-fragmin kinase, an atypical protein kinase with a specialized substrate-binding domain
70. Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine
71. Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2, a key enzyme in angiogenesis
72. Staurosporine-induced conformational changes of cAMP-dependent protein kinase catalytic subunit explain inhibitory potential
73. Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2
74. Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors
75. Structural mechanism for STI-571 inhibition of abelson tyrosine kinase