Targeting thapsigargin towards tumors

Nhu Thi Quynh Doan; Eleonora Sandholdt Paulsen; Pankaj Sehgal; Jesper Vuust Møller; Poul Nissen; Samuel R. Denmeade; John T. Isaacs; Craig A. Dionne; Søren Brøgger Christensen

doi:10.1016/j.steroids.2014.07.009

Targeting thapsigargin towards tumors

Nhu Thi Quynh Doan, Eleonora Sandholdt Paulsen, Pankaj Sehgal, Jesper Vuust Møller, Poul Nissen, Samuel R. Denmeade, John T. Isaacs, Craig A. Dionne, Søren Brøgger Christensen

Research output: Contribution to journal › Review article › peer-review

81 Scopus citations

Abstract

The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin

Original language	English (US)
Pages (from-to)	2-7
Number of pages	6
Journal	Steroids
Volume	97
DOIs	https://doi.org/10.1016/j.steroids.2014.07.009
State	Published - May 2015
Externally published	Yes

Keywords

Prodrug
Prostate specific antigen (PSA)
Prostate specific membrane antigen (PSMA)
Sarco/endoplasmic reticulum (SERCA)
Targeting drugs
Thapsigargin

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Endocrinology
Pharmacology
Clinical Biochemistry
Organic Chemistry

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10.1016/j.steroids.2014.07.009

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@article{423077e6defc4bab996dc50fcb580182,

title = "Targeting thapsigargin towards tumors",

abstract = "The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin",

keywords = "Prodrug, Prostate specific antigen (PSA), Prostate specific membrane antigen (PSMA), Sarco/endoplasmic reticulum (SERCA), Targeting drugs, Thapsigargin",

author = "Doan, {Nhu Thi Quynh} and Paulsen, {Eleonora Sandholdt} and Pankaj Sehgal and M{\o}ller, {Jesper Vuust} and Poul Nissen and Denmeade, {Samuel R.} and Isaacs, {John T.} and Dionne, {Craig A.} and Christensen, {S{\o}ren Br{\o}gger}",

note = "Funding Information: This work has been supported by The Danish Cancer Society, The Danish Research Council for Strategic Research, Carlsbergfondet. Publisher Copyright: {\textcopyright}2014 Elsevier Inc. All rights reserved.",

year = "2015",

month = may,

doi = "10.1016/j.steroids.2014.07.009",

language = "English (US)",

volume = "97",

pages = "2--7",

journal = "Steroids",

issn = "0039-128X",

publisher = "Elsevier Inc.",

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T1 - Targeting thapsigargin towards tumors

AU - Doan, Nhu Thi Quynh

AU - Paulsen, Eleonora Sandholdt

AU - Sehgal, Pankaj

AU - Møller, Jesper Vuust

AU - Nissen, Poul

AU - Denmeade, Samuel R.

AU - Isaacs, John T.

AU - Dionne, Craig A.

AU - Christensen, Søren Brøgger

N1 - Funding Information: This work has been supported by The Danish Cancer Society, The Danish Research Council for Strategic Research, Carlsbergfondet. Publisher Copyright: ©2014 Elsevier Inc. All rights reserved.

PY - 2015/5

Y1 - 2015/5

N2 - The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin

AB - The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin

KW - Prodrug

KW - Prostate specific antigen (PSA)

KW - Prostate specific membrane antigen (PSMA)

KW - Sarco/endoplasmic reticulum (SERCA)

KW - Targeting drugs

KW - Thapsigargin

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U2 - 10.1016/j.steroids.2014.07.009

DO - 10.1016/j.steroids.2014.07.009

M3 - Review article

C2 - 25065587

AN - SCOPUS:84929710977

VL - 97

SP - 2

EP - 7

JO - Steroids

JF - Steroids

SN - 0039-128X

ER -

Targeting thapsigargin towards tumors

Abstract

Keywords

ASJC Scopus subject areas

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