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Thapsigargin--from Thapsia L. to mipsagargin.

Trine Bundgaard Andersen1, Carmen Quiñonero López2, Tom Manczak3

  • 1Department of Plant and Environmental Sciences, Faculty of Science, University of Copenhagen, Thorvaldsensvej 40, 1871 Frederiksberg, Denmark. trba@plen.ku.dk.

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Thapsigargin, a plant compound, inhibits Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) to induce cancer cell death. A new prodrug, Mipsagargin, targets tumor vasculature, showing promise as an anti-cancer therapy.

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Area of Science:

  • Natural Products Chemistry
  • Pharmacology
  • Cancer Biology

Background:

  • Thapsigargin is a sesquiterpene lactone isolated from Thapsia garganica L.
  • Its structure was elucidated in 1985, revealing potent Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) inhibition.
  • SERCA inhibition leads to apoptosis and has been explored for anti-cancer applications.

Purpose of the Study:

  • To review the discovery and development of thapsigargin as an anti-cancer agent.
  • To discuss the mechanism of action and clinical trials of the thapsigargin-derived prodrug, Mipsagargin.
  • To highlight ongoing research into thapsigargin biosynthesis and supply chain development.

Main Methods:

  • Literature review of pharmacological studies, structural elucidation, and clinical trial data.
  • Analysis of thapsigargin's mechanism of action on SERCA and calcium signaling.
  • Exploration of prodrug design and tumor vascular targeting strategies.

Main Results:

  • Thapsigargin effectively inhibits SERCA, inducing apoptosis and tumor necrosis via vascular targeting.
  • The prodrug Mipsagargin (G-202) has undergone initial clinical trials.
  • Research is advancing in understanding thapsigargin biosynthesis and ensuring market supply.

Conclusions:

  • Thapsigargin and its prodrug Mipsagargin represent a promising novel anti-cancer therapeutic strategy.
  • Targeting tumor vasculature with SERCA inhibitors offers a viable approach to solid tumor treatment.
  • Continued research in biosynthesis and production is crucial for clinical availability.