Distinct inhibitory effects of tacrolimus and cyclosporin A on calcineurin phosphatase activity

Journal of Pharmacology and Experimental Therapeutics

Volumn 312, Issue 2, 2005, Pages 816-825

  Fukudo, Masahide ^a   Yano, Ikuko ^a   Masuda, Satohiro ^a   Okuda, Masahiro ^a   Inui, Ken Ichi ^a  

^a KYOTO UNIVERSITY HOSPITAL   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CALCINEURIN; CYCLOSPORIN A; TACROLIMUS;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BODY REGIONS; COMPARTMENT MODEL; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG INHIBITION; DRUG MONITORING; ENZYME ACTIVITY; ENZYME BLOOD LEVEL; ENZYME INHIBITION; HYSTERESIS; MALE; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; RAT;

ANIMALS; CALCINEURIN; CYCLOSPORINE; HALF-LIFE; IMMUNOSUPPRESSIVE AGENTS; MALE; MODELS, BIOLOGICAL; PHOSPHORIC MONOESTER HYDROLASES; RATS; RATS, WISTAR; TACROLIMUS; TISSUE DISTRIBUTION;

EID: 13244279503     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.104.074930     Document Type: Article

References (31)

1. Atkinson K, Britton K, and Biggs J (1984) Distribution and concentration of cyclosporin in human blood. J Clin Pathol 37:1167-1171.
2. Batiuk TD, Kung L, and Halloran PF (1997) Evidence that calcineurin is rate-limiting for primary human lymphocyte activation. J Clin Investig 100:1894-1901.
3. Batiuk TD, Pazderka F, Enns J, DeCastro L, and Halloran PF (1995) Cyclosporine inhibition of calcineurin activity in human leukocytes in vivo is rapidly reversible. J Clin Investig 96:1254-1260.
4. Beal SL, Boeckmann AJ, and Sheiner LB (1992) NONMEM Users Guides. NONMEM Project Group, University of California at San Francisco.
5. Blanchet B, Hulin A, Duvoux C, and Astier A (2003) Determination of serine/threonine protein phosphatase type 2B (PP2B) in lymphocytes by HPLC. Anal Biochem 312:1-6.
6. Bradford MM (1976) A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
7. Caruso R, Perico N, Cattaneo D, Piccinini G, Bonazzola S, Remuzzi G, and Gaspari F (2001) Whole-blood calcineurin activity is not predicted by cyclosporine blood concentration in renal transplant recipients. Clin Chem 47:1679-1687.
8. Clipstone NA and Crabtree GR (1992) Identification of calcineurin as a key signaling enzyme in T-lymphocyte activation. Nature (Lond) 357:695-697.
9. Dumont FJ, Kastner C, lacovone F Jr, and Fischer PA (1994) Quantitative and temporal analysis of the cellular interaction of FK-506 and rapamycin in T-lymphocytes. J Pharmacol Exp Ther 268:32-41.
10. Ford J, Hoggard PG, Owen A, Khoo SH, and Back DJ (2003) A simplified approach to determining P-glycoprotein expression in peripheral blood mononuclear cell subsets. J Immunol Methods 274:129-137.
11. Fruman DA, Klee CB, Bierer BE, and Burakoff SJ (1992) Calcineurin phosphatase activity in T lymphocytes is inhibited by FK506 and cyclosporin A. Proc Natl Acad Sci USA 89:3686-3690.
12. Fruman DA, Pai S-Y, Klee CB, Burakoff SJ, and Bierer BE (1996) Measurement of calcineurin phosphatase activity in cell extracts. Methods 9:146-154.
13. Halloran PF, Helms LM, Kung L, and Noujaim J (1999) The temporal profile of calcineurin inhibition by cyclosporine in vivo. Transplantation 68:1356-1361.
14. Handschumacher RE, Harding MW, Rice J, Drugge RJ, and Speicher DW (1984) Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science (Wash DC) 226:544-547.
15. Hubbard MJ and Klee CB (1991) Exogenous kinases and phosphatases as probes of intracellular modulation, in Molecular Neurobiology: A Practical Approach (Wheal H and Chad J eds) pp 135-157, Oxford University Press, Oxford.
16. Jørgensen KA, Koefoed-Nielsen PB, and Karamperis N (2003) Calcineurin phosphatase activity and immunosuppression: a review on the role of calcineurin phosphatase activity and the immunosuppressive effect of cyclosporin A and tacrolimus. Scand J Immunol 37:93-98.
17. Koefoed-Nielsen PB, Gesualdo MB, Poulsen JH, and Jørgensen KA (2002) Blood tacrolimus levels and calcineurin phosphatase activity early after renal transplantation. Am J Transplant 2:173-178.
18. Kung L, Batiuk TD, Palomo-Pinon S, Noujaim J, Helms LM, and Halloran PF (2001) Tissue distribution of calcineurin and its sensitivity to inhibition by cyclosporine. Am J Transplant 1:325-333.
19. Kung L and Halloran PF (2000) Immunophilins may limit calcineurin inhibition by cyclosporine and tacrolimus at high drug concentrations. Transplantation 70:327-335.
20. Langman LJ, LeGatt DF, Halloran PF, and Yatscoff RW (1996) Pharmacodynamic assessment of mycophenolic acid-induced immunosuppression in renal transplant recipients. Transplantation 62:666-672.
21. Liu J, Albers MW, Wadless TJ, Luan S, Alberg DG, Belshaw PJ, Cohen P, MacKintosh C, Klee CB, and Schreiber SL (1992) Inhibition of T cell signaling by immunophilin-ligand complexes correlates with loss of calcineurin phosphatase activity. Biochemistry 31:3896-3901.
22. Liu J, Farmer JD Jr, Lane WS, Friedman J, Weissman I, and Schreiber SL (1991) Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell 66:807-815.
23. 2 monitoring: a review. Transplantation 73 (Suppl 9):3-11.
24. Ramakrishnan R, DuBois DC, Almon RR, Pyszczynski NA, and Jusko WJ (2002) Fifth-generation model for corticosteroid pharmacodynamics: application to steady-state receptor down-regulation and enzyme induction patterns during seven-day continuous infusion of methylprednisolone in rats. J Pharmacokinet Pharmacodyn 29:1-24.
25. Rusnak F and Mertz P (2000) Calcineurin: form and function. Physiol Rev 80:1483-1521.
26. Sheiner LB, Stanski DR, Vozeh S, Miller RD, and Ham J (1979) Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to d-tubocurarine. Clin Pharmacol Ther 25:358-371.
27. Siekierka JJ, Staruch MJ, Hung SH, and Sigal NH (1989) FK-506, a potent novel immunosuppressive agent, binds to a cytosolic protein which is distinct from the cyclosporin A-binding protein, cyclophilin. J Immunol 143:1580-1583.
28. Staatz CE and Tett SE (2004) Clinical pharmacokinetics and pharmacodynamics of tacrolimus in solid organ transplantation. Clin Pharmacokinet 43:623-653.
29. Su Q, Zhao M, Weber E, Eugster HP, and Ryffel B (1995) Distribution and activity of calcineurin in rat tissues: evidence for post-transcriptional regulation of testis specific calcineurin B. Eur J Biochem 230:469-474.
30. Takada K, Katayama N, Kiriyama A, and Usuda H (1993) Distribution characteristics of immunosuppressants FK506 and cyclosporin A in the blood compartment. Biopharm Drug Dispos 14:659-671.
31. Yatscoff RW, Aspeslet LJ, and Gallant HL (1998) Pharmacodynamic monitoring of immunosuppressive drugs. Clin Chem 44:428-432.