SERCA: Difference between revisions
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== Inhibitors == | == Inhibitors == | ||
SERCA pumps are inhibited by more than 72 compounds<ref>Elam C, Lape M, Deye J, Zultowsky J, Stanton D, Paula S. Discovery of novel SERCA inhibitors by virtual screening of a large compound library. European Journal of Medicinal Chemistry. 2011;46(5):1512-1523.</ref>, however, the most commonly used ones are [[Thapsigargin|thapsigargin]]<ref> | SERCA pumps are inhibited by more than 72 compounds<ref>Elam C, Lape M, Deye J, Zultowsky J, Stanton D, Paula S. Discovery of novel SERCA inhibitors by virtual screening of a large compound library. European Journal of Medicinal Chemistry. 2011;46(5):1512-1523.</ref>, however, the most commonly used ones are [[Thapsigargin|thapsigargin]]<ref>Watson W, Facchina S, Grimaldi M, Verma A. Sarco-endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitors identify a novel calcium pool in the central nervous system. Journal of Neurochemistry. 2003;87(1):30-43.</ref>, [[2,5-Di(tert-butyl)-1,4-benzohydroquinone|2,5-Di(tert-butyl)-1,4-benzohydroquinone]]<ref>http://www.sciencedirect.com/science/article/pii/S0223523411000912</ref> and [[Cyclopiazonic acid|cyclopiazonic acid]]<ref>Moncoq K, Trieber C, Young H. The Molecular Basis for Cyclopiazonic Acid Inhibition of the Sarcoplasmic Reticulum Calcium Pump. Journal of Biological Chemistry. 2007;282(13):9748-9757.</ref>.<br> | ||
== References == | == References == | ||
<references /> | <references /> | ||
Latest revision as of 02:39, 4 December 2017
SERCA is the abbreviation for the sarco/endoplasmic reticulum Ca2+ ATPase pump. It pumps calcium ions into the sarcoplasmic reticulum as well as in the endoplasmic reticulum[1]. It is a regulator of the OFF mechanisms designed to keep our intracellular calcium ion concentration low[2]. SERCA pumps are located on the membrane, they eventually get saturated along with the PMCA pumps by a rising level of calcium ions, and then only do the mitochondria and Na/Ca exchanger begin to work.
Inhibitors
SERCA pumps are inhibited by more than 72 compounds[3], however, the most commonly used ones are thapsigargin[4], 2,5-Di(tert-butyl)-1,4-benzohydroquinone[5] and cyclopiazonic acid[6].
References
- ↑ Heldin, C. and Purton M. (1996) Signal Transduction, 1st edition, London: Chapman and Hall. pp 211
- ↑ Heldin, C. and Purton M. (1996) Signal Transduction, 1st edition, London: Chapman and Hall. pp 210
- ↑ Elam C, Lape M, Deye J, Zultowsky J, Stanton D, Paula S. Discovery of novel SERCA inhibitors by virtual screening of a large compound library. European Journal of Medicinal Chemistry. 2011;46(5):1512-1523.
- ↑ Watson W, Facchina S, Grimaldi M, Verma A. Sarco-endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitors identify a novel calcium pool in the central nervous system. Journal of Neurochemistry. 2003;87(1):30-43.
- ↑ http://www.sciencedirect.com/science/article/pii/S0223523411000912
- ↑ Moncoq K, Trieber C, Young H. The Molecular Basis for Cyclopiazonic Acid Inhibition of the Sarcoplasmic Reticulum Calcium Pump. Journal of Biological Chemistry. 2007;282(13):9748-9757.