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 | |
| State | Published - 2015 |
| Externally published | Yes |
Fingerprint
Keywords
- Prodrug
- Prostate specific antigen (PSA)
- Prostate specific membrane antigen (PSMA)
- Sarco/endoplasmic reticulum (SERCA)
- Targeting drugs
- Thapsigargin
ASJC Scopus subject areas
- Biochemistry
- Clinical Biochemistry
- Endocrinology
- Molecular Biology
- Organic Chemistry
- Pharmacology
- Medicine(all)
Cite this
Targeting thapsigargin towards tumors. / Doan, Nhu Thi Quynh; Paulsen, Eleonora Sandholdt; Sehgal, Pankaj; Møller, Jesper Vuust; Nissen, Poul; Denmeade, Samuel R; Isaacs, John Tod; Dionne, Craig A.; Christensen, Søren Brøgger.
In: Steroids, Vol. 97, 2015, p. 2-7.Research output: Contribution to journal › Article
}
TY - JOUR
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 Tod
AU - Dionne, Craig A.
AU - Christensen, Søren Brøgger
PY - 2015
Y1 - 2015
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
UR - http://www.scopus.com/inward/record.url?scp=84929710977&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84929710977&partnerID=8YFLogxK
U2 - 10.1016/j.steroids.2014.07.009
DO - 10.1016/j.steroids.2014.07.009
M3 - Article
C2 - 25065587
AN - SCOPUS:84929710977
VL - 97
SP - 2
EP - 7
JO - Steroids
JF - Steroids
SN - 0039-128X
ER -