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) |
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Pages (from-to) | 2-7 |
Number of pages | 6 |
Journal | Steroids |
Volume | 97 |
DOIs | |
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