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Review

Thapsigargin—From Traditional Medicine to Anticancer Drug

1
Institute of Organic Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924 Lodz, Poland
2
Department of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2021, 22(1), 4; https://doi.org/10.3390/ijms22010004
Received: 30 November 2020 / Revised: 16 December 2020 / Accepted: 18 December 2020 / Published: 22 December 2020
A sesquiterpene lactone, thapsigargin, is a phytochemical found in the roots and fruits of Mediterranean plants from Thapsia L. species that have been used for centuries in folk medicine to treat rheumatic pain, lung diseases, and female infertility. More recently thapsigargin was found to be a potent cytotoxin that induces apoptosis by inhibiting the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump, which is necessary for cellular viability. This biological activity encouraged studies on the use of thapsigargin as a novel antineoplastic agent, which were, however, hampered due to high toxicity of this compound to normal cells. In this review, we summarized the recent knowledge on the biological activity and molecular mechanisms of thapsigargin action and advances in the synthesis of less-toxic thapsigargin derivatives that are being developed as novel anticancer drugs. View Full-Text
Keywords: thapsigargin; cytotoxin; anticancer activity; sarcoplasmic/endoplasmic reticulum Ca2+ ATPase; unfold protein response; apoptosis; prodrug; prostate-specific antigen; prostate-specific membrane antigen; mipsagargin thapsigargin; cytotoxin; anticancer activity; sarcoplasmic/endoplasmic reticulum Ca2+ ATPase; unfold protein response; apoptosis; prodrug; prostate-specific antigen; prostate-specific membrane antigen; mipsagargin
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MDPI and ACS Style

Jaskulska, A.; Janecka, A.E.; Gach-Janczak, K. Thapsigargin—From Traditional Medicine to Anticancer Drug. Int. J. Mol. Sci. 2021, 22, 4. https://doi.org/10.3390/ijms22010004

AMA Style

Jaskulska A, Janecka AE, Gach-Janczak K. Thapsigargin—From Traditional Medicine to Anticancer Drug. International Journal of Molecular Sciences. 2021; 22(1):4. https://doi.org/10.3390/ijms22010004

Chicago/Turabian Style

Jaskulska, Agata, Anna E. Janecka, and Katarzyna Gach-Janczak. 2021. "Thapsigargin—From Traditional Medicine to Anticancer Drug" International Journal of Molecular Sciences 22, no. 1: 4. https://doi.org/10.3390/ijms22010004

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