Advertisement

Journal of Bioenergetics and Biomembranes

, Volume 37, Issue 6, pp 365–368 | Cite as

Studies of Ca2+ ATPase (SERCA) Inhibition

  • Giuseppe Inesi
  • Suming Hua
  • Cheng Xu
  • Hailun Ma
  • Malini Seth
  • Anand M. Prasad
  • Carlota Sumbilla
Article

 

The Ca2+ transport ATPase of intracellular membranes (SERCA) can be inhibited by a series of chemical compounds such as Thapsigargin (TG), 2,5-di(tert-butyl)hydroquinone (DBHQ) and 1,3-dibromo-2,4,6-tris (methyl-isothio-uronium) benzene (Br2-TITU). These compounds have specific binding sites in the ATPase protein, and different mechanisms of inhibition. On the other hand, SERCA gene silencing offers a convenient and specific method for suppression of SERCA activity in cells. The physiological and pharmacological implications of SERCA inhibition are discussed.

Key Words

SERCA inhibition thapsigargin (TG) 2,5-di(tert-butyl)hydroquinone (DBHQ) 1,3-dibromo-2,4,6-tris (methyl-isothio-uronium) benzene (Br2-TITU) 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Berman, M. C., and Karlish, S. J. (2003). Biochemistry 42, 3556–3566.CrossRefGoogle Scholar
  2. Cavagna, M., O'Donnell, J. M., Sumbilla, C., Inesi, G., and Klein, M. G. (2000). J. Physiol. 258, 53–63.CrossRefGoogle Scholar
  3. Denmeade, S. R., and Isaacs, J. T. (2005). Cancer Biol. 4, 14–22.CrossRefGoogle Scholar
  4. Ghosh, T. K., Bian, J. H., Short, A. D., Rybak, S. L., and Gill, D. L. (1991). J. Biol. Chem. 266, 24690.Google Scholar
  5. Gwathmey, J. K., Copelas, L., MacKinnon, R., Schoen, F. J., Feldman, M. D., Grossman, W., and Morgan, J. P. (1987). Circ. Res. 61, 70–76.Google Scholar
  6. Hua, S., and Inesi, G. (1997). Biochemistry 36, 11865–11872.CrossRefGoogle Scholar
  7. Hua, S., Malak, H., Lakowicz, J. R., and Inesi, G. (1995). Biochemistry 34, 5137–5142.CrossRefGoogle Scholar
  8. Hua, S., Xu, C., Ma, H., and Inesi, G. (2005). J. Biol. Chem. 280,17579–17583.CrossRefGoogle Scholar
  9. Im, S. H., and Rao, A. (2004). Mol. Cell 18, 1–9.Google Scholar
  10. Kirby, M. S., Sagara, Y., Gaa, S., Inesi, G., Lederer, W. J., and Rogers, T. B. (1992). J. Biol. Chem. 267, 12545–12551.Google Scholar
  11. MacLennan, D. H., Brandl, C. J., Korczak, B., and Green, N. M. (1985). Nature 316, 696–700.CrossRefGoogle Scholar
  12. Molkentin, J. D. (2004). Cardiovasc. Res. 63, 467–465.CrossRefGoogle Scholar
  13. Nykanen, A., Haley, B., and Zamore, P. D. (2001). Cell 107, 309–321.CrossRefGoogle Scholar
  14. Olson, E. N., and Williams, R. S. (2000). Bioesseays 22, 510–519.CrossRefGoogle Scholar
  15. Sagara, Y., and Inesi, G. (1991). J. Biol. Chem. 266, 13503–13506.Google Scholar
  16. Seth, M., Sumbilla, C., Mullen, S. P., Lewis, D., Klein, M. G., Hussain, A., Soboloff, J., Gill, D. L., and Inesi, G. (2004). Proc. Natl. Acad. Sci. U.S.A. 101, 16683–16688.CrossRefGoogle Scholar
  17. Rasmussem, U., Christensen, S. B., and Sandber, F. (1978). Acta Pharmac. Suec. 15, 133–140.Google Scholar
  18. Sorensen, T. L., Moller, J. V., and Nissen, P. (2004). Science 304, 1672–1675.CrossRefGoogle Scholar
  19. Toyoshima, C., Nakasako, M., Nomura, H., and Ogawa, H. (2000). Nature 405, 647–655.CrossRefGoogle Scholar
  20. Toyoshima, C., and Nomura, H. (2002). Nature 418, 605–611.CrossRefGoogle Scholar
  21. Toyoshima, C., Nomura, H., and Tsuda, T. (2004). Nature 432, 361–368.CrossRefGoogle Scholar
  22. Treiman, M., Caspersen, C., and Christensen, S. B. (1998). Trends Pharmacol. Sci. 19, 131–135.CrossRefGoogle Scholar
  23. Vega, R. B., Bassel-Duby, R., and Olson, E. N. (2003). J. Biol. Chem. 278, 36981–36984.CrossRefGoogle Scholar
  24. Williams, R. S., and Rosenberg, P. (2002). Cold Spring Harbor Symp. Quant. Biol. 67, 339–344.CrossRefGoogle Scholar
  25. Xu, C., Ma, H., Inesi, G., Al-Shawi, M. K., and Toyoshima, C. J. (2004). Biol. Chem. 279, 17973–17979.CrossRefGoogle Scholar
  26. Yu, M., Lin, J., Khadeer, M., Yeh, Y., Inesi, G., and Hussain, A. (1999). Arch. Biochem. Biophys. 362, 225–232.CrossRefGoogle Scholar
  27. Zhong, L., and Inesi, G. (1998). J. Biol. Chem. 273, 12994–12998.CrossRefGoogle Scholar

Copyright information

© Springer Science + Business Media, Inc. 2005

Authors and Affiliations

  • Giuseppe Inesi
    • 1
  • Suming Hua
    • 1
  • Cheng Xu
    • 1
  • Hailun Ma
    • 1
  • Malini Seth
    • 1
  • Anand M. Prasad
    • 1
  • Carlota Sumbilla
    • 1
  1. 1.Department of Biochemistry and Molecular BiologyUniversity of Maryland School of MedicineBaltimore

Personalised recommendations