The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca(2+) 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.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4696022 | PMC |
| http://dx.doi.org/10.1016/j.steroids.2014.07.009 | DOI Listing |
Publication Analysis
Top Keywords
prostate specific
8
targeting thapsigargin
4
thapsigargin tumors
4
tumors skin
4
skin irritating
4
irritating principle
4
principle thapsia
4
thapsia garganica
4
garganica isolated
4
isolated named
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!