Targeting thapsigargin towards tumors

Nhu Thi Quynh Doan, Eleonora Sandholdt Paulsen, Pankaj Sehgal, Jesper Vuust Møller, Poul Nissen, Samuel R. Denmeade, John T. Isaacs, Craig A. Dionne, Søren Brøgger Christensen

Research output: Contribution to journalReview articlepeer-review

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 languageEnglish (US)
Pages (from-to)2-7
Number of pages6
JournalSteroids
Volume97
DOIs
StatePublished - May 2015
Externally publishedYes

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

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