Thapsigargin

Chembox new
Name = Thapsigargin
ImageFile = Thapsigargin.png ImageName = Thapsigargin
Section1 = Chembox Identifiers
CASNo = 67526-95-8
Section2 = Chembox Properties
Formula = C₃₄H₅₀O_{12
MolarMass = 650.76 g/mol}

Thapsigargin is a tight-binding inhibitor of a class of enzymes known by the acronym SERCA, which stands for sarco / endoplasmic reticulum Ca²⁺ ATPase. [cite journal |author=Rogers TB, Inesi G, Wade R, Lederer WJ |title=Use of thapsigargin to study Ca2+ homeostasis in cardiac cells |journal=Biosci. Rep. |volume=15 |issue=5 |pages=341–9 |year=1995 |pmid=8825036 |doi=10.1007/BF01788366] 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"). [cite journal |author=Golenser J, Waknine JH, Krugliak M, Hunt NH, Grau GE |title=Current perspectives on the mechanism of action of artemisinins |journal=Int. J. Parasitol. |volume=36 |issue=14 |pages=1427–41 |year=2006 |pmid=17005183 |doi=10.1016/j.ijpara.2006.07.011]

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.

References

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. [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9288732&dopt=Abstract PMID:9288732]
* Ibaraki N (1997). "A brighter future for cataract surgery." "Nat Med." 3(9):958-60. [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9288718&dopt=Abstract PMID:9288718]

External links

* [http://www.fermentek.co.il/thapsigargin.htm Thapsigargin product page] from Fermentek.