Everything about Thapsigargin totally explained
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Thapsigargin is a tight-binding
inhibitor of a class of
enzymes known by the acronym
SERCA, which stands for
sarco /
endoplasmic reticulum Ca2+ ATPase. 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).
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.
Further Information
Get more info on 'Thapsigargin'.
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