Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development.

Research output: Contribution to journalReviewResearchpeer-review

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Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development. / Doan, Thi Quynh Nhu; Christensen, Søren Brøgger.

In: Current Pharmaceutical Design, Vol. 21, No. 38, 10.2015, p. 5505-5517.

Research output: Contribution to journalReviewResearchpeer-review

Harvard

Doan, TQN & Christensen, SB 2015, 'Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development.', Current Pharmaceutical Design, vol. 21, no. 38, pp. 5505-5517. https://doi.org/10.2174/1381612821666151002112824

APA

Doan, T. Q. N., & Christensen, S. B. (2015). Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development. Current Pharmaceutical Design, 21(38), 5505-5517. https://doi.org/10.2174/1381612821666151002112824

Vancouver

Doan TQN, Christensen SB. Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development. Current Pharmaceutical Design. 2015 Oct;21(38):5505-5517. https://doi.org/10.2174/1381612821666151002112824

Author

Doan, Thi Quynh Nhu ; Christensen, Søren Brøgger. / Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development. In: Current Pharmaceutical Design. 2015 ; Vol. 21, No. 38. pp. 5505-5517.

Bibtex

@article{490bf1663d324567b444a65248887dd4,
title = "Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development.",
abstract = "Thapsigargin was originally isolated from the roots of the Mediterranean umbelliferous plant Thapsia garganica in order to characterize the skin irritant principle. 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 design of an equipotent analogue containing a linker. Conjugation of a peptide, which only is a substrate for prostate specific antigen enabled design of a prodrug (G115) targeted against prostate cancer. Conjugation to a peptide, which only is a substrate for prostate specific membrane antigen enabled development of a prodrug (G202), which is targeted towards a number of cancer diseases including hepatocellular carcinoma. G202 has under the name of mipsagargin in clinical trials 2 shown promising properties against hepatocellular carcinoma.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "Doan, {Thi Quynh Nhu} and Christensen, {S{\o}ren Br{\o}gger}",
year = "2015",
month = "10",
doi = "10.2174/1381612821666151002112824",
language = "English",
volume = "21",
pages = "5505--5517",
journal = "Current Pharmaceutical Design",
issn = "1381-6128",
publisher = "Bentham Science Publishers",
number = "38",

}

RIS

TY - JOUR

T1 - Thapsigargin, origin, chemistry, structure-activity relationships and prodrug development.

AU - Doan, Thi Quynh Nhu

AU - Christensen, Søren Brøgger

PY - 2015/10

Y1 - 2015/10

N2 - Thapsigargin was originally isolated from the roots of the Mediterranean umbelliferous plant Thapsia garganica in order to characterize the skin irritant principle. 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 design of an equipotent analogue containing a linker. Conjugation of a peptide, which only is a substrate for prostate specific antigen enabled design of a prodrug (G115) targeted against prostate cancer. Conjugation to a peptide, which only is a substrate for prostate specific membrane antigen enabled development of a prodrug (G202), which is targeted towards a number of cancer diseases including hepatocellular carcinoma. G202 has under the name of mipsagargin in clinical trials 2 shown promising properties against hepatocellular carcinoma.

AB - Thapsigargin was originally isolated from the roots of the Mediterranean umbelliferous plant Thapsia garganica in order to characterize the skin irritant principle. 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 design of an equipotent analogue containing a linker. Conjugation of a peptide, which only is a substrate for prostate specific antigen enabled design of a prodrug (G115) targeted against prostate cancer. Conjugation to a peptide, which only is a substrate for prostate specific membrane antigen enabled development of a prodrug (G202), which is targeted towards a number of cancer diseases including hepatocellular carcinoma. G202 has under the name of mipsagargin in clinical trials 2 shown promising properties against hepatocellular carcinoma.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.2174/1381612821666151002112824

DO - 10.2174/1381612821666151002112824

M3 - Review

VL - 21

SP - 5505

EP - 5517

JO - Current Pharmaceutical Design

JF - Current Pharmaceutical Design

SN - 1381-6128

IS - 38

ER -

ID: 147231787