Targeting thapsigargin towards tumors

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 - 2015/5

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.

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.

U2 - 10.1016/j.steroids.2014.07.009

DO - 10.1016/j.steroids.2014.07.009

M3 - Journal article

C2 - 25065587

SN - 0039-128X

VL - 97

SP - 2

EP - 7

JO - Steroids

JF - Steroids

ER -