X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex

Cell

Volumn 82, Issue 3, 1995, Pages 507-522

  Griffith, James P ^a   Kim, Joseph L ^a   Kim, Eunice E ^a   Sintchak, Michael D ^a   Thomson, John A ^a   Fitzgibbon, Matthew J ^a   Fleming, Mark A ^a   Caron, Paul R ^a   Hsiao, Kathy ^a   Navia, Manuel A ^a  

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCINEURIN; CALCINEURIN A; CALCINEURIN B; FKBP 12; IMMUNOPHILIN; PHOSPHATASE; TACROLIMUS; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CATTLE; CYTOARCHITECTURE; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME STRUCTURE; IMMUNOSUPPRESSIVE TREATMENT; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; X RAY ANALYSIS;

ANIMALIA; BOS TAURUS;

EID: 0029133116     PISSN: 00928674     EISSN: None     Source Type: Journal    
DOI: 10.1016/0092-8674(95)90439-5     Document Type: Article

References (75)

1. Charged surface residues of FKBP12 participate in formation of the FKBP12-FK506-calcineurin complex
2. Amino-terminal myristoylation induces cooperative calcium binding to recoverin
3. Structure of calmodulin refined at 2.2 Å resolution
4. FK506-binding protein: three-dimensional structure of the complex with the antagonist L-685,818
5. Two distinct signal transmission pathways in T lymphocytes are inhibited by complexes formed between and immunophilin and either FK506 or rapamycin
6. Pharmacology of cyclosporine (Sandimmune). IV. Pharmacological properties in vivo
7. Biological effects of cyclosporin A: a new antilymphocytic agent
8. Free R value: a novel statistical quantity for assessing the accuracy of crystal structures
9. RIBBONS 2.0
10. The CCP4 suite: programs for protein crystallography
11. Identification of calcineurin as a key signaling enzyme in T-lymphocyte activation
12. The structure and regulation of protein phosphatases
13. Protein phosphatases come of age
14. Contingent genetic regulatory events in T lymphocyte activation
15. Signal transmission between the plasma membrane and nucleus of T lymphocytes
16. Dephosphorylation of phosphopeptides by calcineurin (protein phosphatase 2B)
17. Pharmacology of CsA and FK-506
18. The immunosuppressive and toxic effects of FK-506 are mechanistically related: pharmacology of a novel antagonist of FK-506 and rapamycin
19. Cyclosporin A specifically inhibits function of nuclear proteins involved in T cell activation
20. Three-dimensional structure of recoverin, a calcium sensor in vision
21. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A
22. FK506 binding protein mutational analysis
23. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK506 and cyclosporin A
24. Protein N-myristoylation
25. The medicinal chemistry of FK-506
26. Cloning of human calcineurin A: evidence for two isozymes and identification of a polyproline structural domain
27. Identification of an autoinhibitory domain in calcineurin
28. The FK506-binding protein proline rotamase is a target for the immunosuppressive agent FK506 in Saccharomyces cerevisiae
29. Protein kinases and phosphatases: the yin and yang of protein phosphorylation and signaling
30. Solution structure of a calmodulin-target peptide complex by multidimensional NMR
31. The complete primary structure of calcineurin A, a calmodulin binding protein homologous with protein phosphatases 1 and 2A
32. Conformation of FK506 in X-ray structures of its complexes with human recombinant FKBP12 mutants
33. p is a substrate for calcineurin and interacts with Fos and Jun
34. Characterization of the calcium-binding sites of calcineurin B
35. Characterization of a cDNA clone encoding the calmodulin-binding domain of mouse brain calcineurin
36. Cloning and characterization of molecular isoforms of the catalytic subunit of calcineurin using nonisotopic methods
37. The calmodulin-dependent activation and deactivation of the phosphoprotein phosphatase, calcineurin, and the effect of nucleotides, pyrophosphate, and divalent metal ions
38. FK-506, a novel immunosuppressant isolated from Streptomyces. I. Fermentation, isolation and physico-chemical and biological characteristics
39. Calcineurin
40. Rapamycin sensitivity in Saccharomyces cerevisiae is mediated by a peptidyl-prolyl clstrans isomerase related to human FK506-binding protein
41. Carp muscle calcium-binding protein II Structure determination and general description
42. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes
43. Isotope effects on the mechanism of calcineurin catalysis: kinetic isotope and isotope exchange studies
44. p, a T lymphocyte DNA-binding protein that is a target for calcineurin and immunosuppressive drugs
45. Target enzyme recognition by calmodulin: 2.4 Å structure of a calmodulin-peptide complex
46. The latch region of calcineurin B is involved in both immunosuppresssant-immunophilin complex docking and phosphatase activation
47. Structure and function of the multifunctional DNA-repair enzyme exonuclease III
48. Purple acid phosphatase a diiron enzyme that catalyzes a direct phospho group transfer to water
49. Isolation and characterization of a cDNA clone coding for the calcium-binding subunit of calcineurin from bovine brain: an identical amino acid sequence to the human protein
50. Protein folding and association: insights from the interfacial and thermodynamic properties of hydrocarbons
51. Characterization of the nuclear and cytoplasmic components of the lymphoid-specific nuclear factor of activated T-cells (NF-AT) complex
52. Crystallographic refinement and structure of DNase I at 2 Å resolution
53. FK-506- and CsA-sensitive activation of the interleukin-2 promoter by calcineurin
54. Maximum likelihood refinement of heavy atom parameters
55. Calcium regulation of calcineurin phosphatase activity by its B subunit and calmodulin: role of the autoinhibitory domain
56. Improved Fourier coefficients for maps using phases from partial structures with errors
57. Myristylation and palmitylation of Src family members: the fats of the matter
58. Protein serine/threonine phosphatases: new avenues for cell regulation
59. Cyclosporin A, FK-506, and rapamycin: pharmacologic probes of lymphocyte signal transduction
60. Calcineurin subunit interactions mapping the calcineurin B binding domain on calcineurin A
61. 2+-dependent phosphorylation and dephosphorylation of a 63-kDa subunit-containing bovine brain calmodulin-stimulated cyclic nucleotide phosphodiesterase isozyme
62. Crystal structure of purple-acid phosphatase containing a dinuclear Fe(III)-Zn(II) active site
63. Unbiased three-dimensional refinement of heavy-atom parameters by correlation of origin-removed Patterson functions
64. The immunosuppressant FK506 selectively inhibits expression of early T cell activation genes
65. Atomic structure of FKBP-FK506, an immunophilin-immunosupressant complex
66. Atomic structure of the rapamycin human immunophilin FKBP-12 complex
67. Atomic structures of human immunophilin FKBP12 complexes with FK506 and rapamycin
68. Rapamycin (AY-22,989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle
69. Resolution of phase ambiguity in macromolecular crystallography
70. Comparative X-ray structures of the major binding protein for the immunosuppressant FK506 (tacrolimus) in unliganded form and in complex with FK506 and rapamycin
71. A composite FKBP12-FK506 surface that contacts calcineurin
72. N-myristylation of the catalytic subunit of cAMP-dependent protein kinase conveys structural stability
73. The use of Sayre's equation with solvent flattening and histogram matching for phase extension and refinement of protein structures
74. Mutational analysis of a Ser/Thr phosphatase: identification of residues important in phosphoesterase substrate binding and catalysis