Effects of cyclosporin A, FK506 and rapamycin on calcineurin phosphatase activity in mouse brain

IUBMB Life

Volumn 58, Issue 7, 2006, Pages 429-433

  Yu, Da Yu ^a   Luo, Jing ^a   Bu, Fan ^a   Zhang, Wen ^a   Wei, Qun ^a  

^a BEIJING NORMAL UNIVERSITY   (China)

Author keywords

Catalytic mechanism; Enzyme mechanisms; Enzymology; Protein structure; Substrate and inhibitor recognition enzyme inhibitors as drugs

Indexed keywords

CALCINEURIN; CYCLOSPORIN A; PHOSPHATASE; PROTEIN KINASE (CALCIUM,CALMODULIN); RAPAMYCIN; TACROLIMUS;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BRAIN METABOLISM; COMPETITIVE INHIBITION; COMPLEX FORMATION; CONTROLLED STUDY; DRUG EFFECT; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME KINETICS; ENZYME MECHANISM; LATERAL BRAIN VENTRICLE; MALE; MOUSE; NONHUMAN; PROTEIN STRUCTURE;

ANIMALS; BRAIN; CALCINEURIN; CYCLOSPORINE; MALE; MICE; MICE, INBRED BALB C; PHOSPHORIC MONOESTER HYDROLASES; SIROLIMUS; TACROLIMUS;

EID: 33745684082     PISSN: 15216543     EISSN: 15216551     Source Type: Journal    
DOI: 10.1080/15216540600791555     Document Type: Article

References (17)

1. Hubbard, M. J., and Klee, C. B. (1989) Functional domain structure of calcineurin A: mapping by limited proteolysis. Biochemistry 28, 1868-1874.
2. Xiang, B. Q., Liu, P., Jiang, G. H., Zou, K., Yi, F., Yang, S. J., and Wei, Q. (2003) The catalytically active domain in the A subunit of calcineurin. Biol. Chem. 384, 1429-1434.
3. Rusnak, F., and Mertz, P. (2000) Calcineurin: form and function. Physiol. Rev. 80, 1483-1521.
4. Wei, Q., Holzer, M., Brueckner, M. K., Liu, Y., and Arendt, T. (2002). Dephosphorylation of tau protein by calcineurin triturated into neural living cells. Cell Mol. Neurobiol. 22, 13-24.
5. Li, H., and Wei, Q. (2001) Conformation changes in brain calcineurin in diabetic rats with or without treatment with vanadyl sulfate. IUBMB Life 51, 373-376.
6. Liu, J., Farmer Jr, J. D., Lane, W. S., Friedman, J., Weissman, I., and Schreiber, S. L. (1991) Calcineurin is a common target of cyclophilin- cyclosporin A and FKBP-FK506 complexes. Cell 66, 807-815.
7. Perrino, B. A., Wilson, A. J., Ellison, P., and Clapp, L. H. (2002) Substrate selectivity and sensitivity to inhibition by FK506 and cyclosporin A of calcineurin heterodimers composed of the {alpha} or {beta} catalytic subunit. FEBS J. 269, 3540-3548.
8. Bierer, B. E., Mattila, P. S., Standaert, R. F., Herzenberg, L. A., Burakoff, S. J., Crabtree, G. R., and Schreiber, S. L. (1990) Two distinct signal transmission pathways in T lymphocytes are inhibited by complexes formed between an immunophilin and either FK506 or rapamycin. Proc. Natl. Acad. Sci. USA 87, 9231-9235.
9. Bennett, P. C., Zhao, W. Q., Lawen, A., and Ng, K. T. (1996) Cyclosporin A, an inhibitor of calcineurin, impairs memory formation in day-old chicks. Brain Res. 73, 107-117.
10. Perrino, B. A., Fong, Y. L., Brickey, D. A., Saitoh, Y., Ushio, Y., Fukunaga, K., Miyamoto, E., and Soderling, T. R. (1992) Characterization of the phosphatase activity of a baculovirus-expressed calcineurin A isoform. J. Biol. Chem. 267, 15965-15969.
11. Yan, L. J., and Wei, Q. (1999) High activity of the calcineurin A subunit with a V314 deletion. Biol. Chem. 380, 1281-1285.
12. Griffith, J. P., Kim, J. L., Kim, E. E., Sintchak, M. D., Thomson, J. A., Fitzgibbon, M. J., Fleming, M. A., Caron, P. R., Hsiao, K., and Navia, M. A. (1995) X-ray structure of calcineurin inhibited by the immunophilin- immunosuppressant FKBP12-FK506 complex. Cell 82, 507-522.
13. Jin, L., and Harrison, S. C. (2002) Crystal structure of human calcineurin complexed with cyclosporin A and human cyclophilin. Proc. Natl. Acacl. Sci. USA 99, 13522-13526.
14. Etzkorn, F. A., Chang, Z. Y., Stolz, L. A., and Walsh, C. T. (1994) Cyclophilin residues that affect noncompetitive inhibition of the protein serine phosphatase activity of calcineurin by the cyclophilin-cyclosporin A complex. Biochemistry 33, 2380-2388.
15. Dumont, F. J., Staruch, M. J., Koprak, S. L., Siekierka, J. J., Lin, C. S., Harrison, R., Sewell, T., Kindt, V. M., Beattie, T. R., and Wyvratt, M. (1992) The immunosuppressive and toxic effects of FK-506 are mechanistically related: pharmacology of a novel antagonist of FK-506 and rapamycin. J. Exp. Meet. 176, 751-760.
16. Chan, C. P., Gallis, B., Blumenthal, D. K., Pallen, C. J., Wang, J. H., and Krebs, E. G. (1986) Characterization of the phosphotyrosyl protein phosphatase activity of calmodulin-dependent protein phosphatase. J. Biol. Chem. 261, 9890-9895.
17. Cardenas, M. E., Muir, R. S., Breuder, T., and Heitman, J. (1995) Targets of immunophilin- immunosuppressant complexes are distinct highly conserved regions of calcineurin A. EMBO J. 14, 2772-2783.