Thapsigargin - from Thapsia L. to Mipsagargin

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Standard

Thapsigargin - from Thapsia L. to Mipsagargin. / Andersen, Trine Bundgaard; Quinonero Lopez, Carmen; Manczak, Tom; Martinez, Karen Agatha; Simonsen, Henrik Toft.

I: Molecules, Bind 20, Nr. 4, 2015, s. 6113-6127.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Andersen, TB, Quinonero Lopez, C, Manczak, T, Martinez, KA & Simonsen, HT 2015, 'Thapsigargin - from Thapsia L. to Mipsagargin', Molecules, bind 20, nr. 4, s. 6113-6127. https://doi.org/10.3390/molecules20046113

APA

Andersen, T. B., Quinonero Lopez, C., Manczak, T., Martinez, K. A., & Simonsen, H. T. (2015). Thapsigargin - from Thapsia L. to Mipsagargin. Molecules, 20(4), 6113-6127. https://doi.org/10.3390/molecules20046113

Vancouver

Andersen TB, Quinonero Lopez C, Manczak T, Martinez KA, Simonsen HT. Thapsigargin - from Thapsia L. to Mipsagargin. Molecules. 2015;20(4):6113-6127. https://doi.org/10.3390/molecules20046113

Author

Andersen, Trine Bundgaard ; Quinonero Lopez, Carmen ; Manczak, Tom ; Martinez, Karen Agatha ; Simonsen, Henrik Toft. / Thapsigargin - from Thapsia L. to Mipsagargin. I: Molecules. 2015 ; Bind 20, Nr. 4. s. 6113-6127.

Bibtex

@article{4cdda8add7034d0aa27c920a7abfa511,
title = "Thapsigargin - from Thapsia L. to Mipsagargin",
abstract = "The sesquiterpene lactone thapsigargin is found in the plant Thapsia garganica L., and is one of the major constituents of the roots and fruits of this Mediterranean species. In 1978, the first pharmacological effects of thapsigargin were established and the full structure was elucidated in 1985. Shortly after, the overall mechanism of the Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) inhibition that leads to apoptosis was discovered. Thapsigargin has a potent antagonistic effect on the SERCA and is widely used to study Ca2+-signaling. The effect on SERCA has also been utilized in the treatment of solid tumors. A prodrug has been designed to target the blood vessels of cancer cells; the death of these blood vessels then leads to tumor necrosis. The first clinical trials of this drug were initiated in 2008, and the potent drug is expected to enter the market in the near future under the generic name Mipsagargin (G-202). This review will describe the discovery of the new drug, the on-going elucidation of the biosynthesis of thapsigargin in the plant and attempts to supply the global market with a novel potent anti-cancer drug.",
author = "Andersen, {Trine Bundgaard} and {Quinonero Lopez}, Carmen and Tom Manczak and Martinez, {Karen Agatha} and Simonsen, {Henrik Toft}",
year = "2015",
doi = "10.3390/molecules20046113",
language = "English",
volume = "20",
pages = "6113--6127",
journal = "Molecules",
issn = "1420-3049",
publisher = "M D P I AG",
number = "4",

}

RIS

TY - JOUR

T1 - Thapsigargin - from Thapsia L. to Mipsagargin

AU - Andersen, Trine Bundgaard

AU - Quinonero Lopez, Carmen

AU - Manczak, Tom

AU - Martinez, Karen Agatha

AU - Simonsen, Henrik Toft

PY - 2015

Y1 - 2015

N2 - The sesquiterpene lactone thapsigargin is found in the plant Thapsia garganica L., and is one of the major constituents of the roots and fruits of this Mediterranean species. In 1978, the first pharmacological effects of thapsigargin were established and the full structure was elucidated in 1985. Shortly after, the overall mechanism of the Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) inhibition that leads to apoptosis was discovered. Thapsigargin has a potent antagonistic effect on the SERCA and is widely used to study Ca2+-signaling. The effect on SERCA has also been utilized in the treatment of solid tumors. A prodrug has been designed to target the blood vessels of cancer cells; the death of these blood vessels then leads to tumor necrosis. The first clinical trials of this drug were initiated in 2008, and the potent drug is expected to enter the market in the near future under the generic name Mipsagargin (G-202). This review will describe the discovery of the new drug, the on-going elucidation of the biosynthesis of thapsigargin in the plant and attempts to supply the global market with a novel potent anti-cancer drug.

AB - The sesquiterpene lactone thapsigargin is found in the plant Thapsia garganica L., and is one of the major constituents of the roots and fruits of this Mediterranean species. In 1978, the first pharmacological effects of thapsigargin were established and the full structure was elucidated in 1985. Shortly after, the overall mechanism of the Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) inhibition that leads to apoptosis was discovered. Thapsigargin has a potent antagonistic effect on the SERCA and is widely used to study Ca2+-signaling. The effect on SERCA has also been utilized in the treatment of solid tumors. A prodrug has been designed to target the blood vessels of cancer cells; the death of these blood vessels then leads to tumor necrosis. The first clinical trials of this drug were initiated in 2008, and the potent drug is expected to enter the market in the near future under the generic name Mipsagargin (G-202). This review will describe the discovery of the new drug, the on-going elucidation of the biosynthesis of thapsigargin in the plant and attempts to supply the global market with a novel potent anti-cancer drug.

U2 - 10.3390/molecules20046113

DO - 10.3390/molecules20046113

M3 - Journal article

C2 - 25856061

VL - 20

SP - 6113

EP - 6127

JO - Molecules

JF - Molecules

SN - 1420-3049

IS - 4

ER -

ID: 135531107