Targeting thapsigargin towards tumors

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

Research output: Contribution to journalArticle

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 - 2015
Externally publishedYes

Fingerprint

Thapsigargin
Prodrugs
Tumors
Thapsia
Sarcoplasmic Reticulum Calcium-Transporting ATPases
Neoplasms
Prostate-Specific Antigen
Prostatic Neoplasms
Skin
Cells
Clinical Trials
Tissue
Apoptosis
Peptides
Substrates

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

Doan, N. T. Q., Paulsen, E. S., Sehgal, P., Møller, J. V., Nissen, P., Denmeade, S. R., ... Christensen, S. B. (2015). Targeting thapsigargin towards tumors. Steroids, 97, 2-7. https://doi.org/10.1016/j.steroids.2014.07.009

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 journalArticle

Doan, NTQ, Paulsen, ES, Sehgal, P, Møller, JV, Nissen, P, Denmeade, SR, Isaacs, JT, Dionne, CA & Christensen, SB 2015, 'Targeting thapsigargin towards tumors', Steroids, vol. 97, pp. 2-7. https://doi.org/10.1016/j.steroids.2014.07.009
Doan NTQ, Paulsen ES, Sehgal P, Møller JV, Nissen P, Denmeade SR et al. Targeting thapsigargin towards tumors. Steroids. 2015;97:2-7. https://doi.org/10.1016/j.steroids.2014.07.009
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. / Targeting thapsigargin towards tumors. In: Steroids. 2015 ; Vol. 97. pp. 2-7.
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