Thapsigargin, Origin, Chemistry, Structure-Activity Relationships and Prodrug Development.

  title={Thapsigargin, Origin, Chemistry, Structure-Activity Relationships and Prodrug Development.},
  author={Nhu Thi Quynh Doan and S\oren Br\ogger Christensen},
  journal={Current pharmaceutical design},
  volume={21 38},
Thapsigargin was originally isolated from the roots of the Mediterranean umbelliferous plant Thapsia garganica in order to characterize the skin irritant principle. Characteristic chemical properties and semi-syntheses are reviewed. The biological activity was related to the subnanomolar affinity for the sarco/endoplasmic reticulum calcium ATPase. Prolonged inhibition of the pump afforded collapse of the calcium homeostasis and eventually apoptosis. Structure-activity relationships enabled… CONTINUE READING


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