Thapsigargin

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Thapsigargin
Thapsigargin
Identifiers
CAS number [67526-95-8]
Properties
Molecular formula C34H50O12
Molar mass 650.76 g/mol
Except where noted otherwise, data are given for
materials in their standard state
(at 25 °C, 100 kPa)
Infobox disclaimer and references

Thapsigargin is a tight-binding inhibitor of a class of enzymes known by the acronym SERCA, which stands for sarco / endoplasmic reticulum Ca2+ ATPase.[1] Structurally, thapsigargin is classified as a sesquiterpene lactone, and is extracted from a plant, Thapsia garganica. It is a tumor promoter in mammalian cells. The structural similarity of thapsigargin with the anti-malarial drug, artemesinin, led to a proposal that this class of drugs acts on SERCA within the malaria parasite (for example, the human malaria parasite, Plasmodium falciparum).[2]

Thapsigargin raises cytosolic calcium concentration by blocking the ability of the cell to pump calcium into the sarcoplasmic and endoplasmic reticula which causes these stores to become depleted. Store-depletion can secondarily activate plasma membrane calcium channels, allowing an influx of calcium into the cytosol.

Thapsigargin is useful in experimentation examining the impacts of increasing cytosolic calcium concentrations.

Potential medical uses of Thapsigargin

Thapsigagrin is mentioned as a possible treatment for posterior capsular opacification.

[edit] References

 The references in this article would be clearer with a different or consistent style of citation, footnoting, or external linking.
  1. ^ Rogers TB, Inesi G, Wade R, Lederer WJ (1995). "Use of thapsigargin to study Ca2+ homeostasis in cardiac cells". Biosci. Rep. 15 (5): 341-9. doi:10.1007/BF01788366. PMID 8825036. 
  2. ^ Golenser J, Waknine JH, Krugliak M, Hunt NH, Grau GE (2006). "Current perspectives on the mechanism of action of artemisinins". Int. J. Parasitol. 36 (14): 1427-41. doi:10.1016/j.ijpara.2006.07.011. PMID 17005183. 

[edit] Further reading

  • Duncan G, Wormstone IM, Liu CS, Marcantonio JM, Davies PD (1997). "Thapsigargin-coated intraocular lenses inhibit human lens cell growth." Nat Med. 3(9):1026-8. PMID:9288732
  • Ibaraki N (1997). "A brighter future for cataract surgery." Nat Med. 3(9):958-60. PMID:9288718

[edit] External links

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