Targeting thapsigargin towards tumors
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Targeting thapsigargin towards tumors. / Christensen, Søren Brøgger; Doan, Thi Quynh Nhu; Paulsen, Eleonora Sandholdt; Sehgal, Pankaj; Møller, Jesper Vuust; Nissen, Poul; Denmeade, Samuel R.; Isaacs, John T.; Dionne, Craig A.
In: Steroids, Vol. 97, 2015, p. 2-7.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Targeting thapsigargin towards tumors
AU - Christensen, Søren Brøgger
AU - Doan, Thi Quynh Nhu
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
PY - 2015
Y1 - 2015
N2 - The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structureelucidated. By inhibiting the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) thapsigargin provokesapoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for eitherprostate 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 iscurrently 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 structureelucidated. By inhibiting the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) thapsigargin provokesapoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for eitherprostate 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 iscurrently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin.
U2 - 10.1016/j.steroids.2014.07.009
DO - 10.1016/j.steroids.2014.07.009
M3 - Journal article
C2 - 25065587
VL - 97
SP - 2
EP - 7
JO - Steroids
JF - Steroids
SN - 0039-128X
ER -
ID: 162907761