Targeting thapsigargin towards tumors

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  • Nhu Thi Quynh Doan, Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen Ø, Denmark., Ukendt
  • Eleonora Sandholdt Paulsen
  • Pankaj Sehgal
  • Jesper Vuust Møller
  • Poul Nissen
  • Samuel R Denmeade, The Bunting-Blaustein Cancer Research Building, 1650 Orleans Street, Baltimore, MD 21231, USA.
  • ,
  • John T Isaacs, The Bunting-Blaustein Cancer Research Building, 1650 Orleans Street, Baltimore, MD 21231, USA.
  • ,
  • Craig A Dionne, GenSpera, 2511 N Loop 1604 W, Suite 204, San Antonio, TX 78258, USA.
  • ,
  • Søren Brøgger Christensen, Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen Ø, Denmark. Electronic address: soren.christensen@sund.ku.dk., Danmark

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.

OriginalsprogEngelsk
TidsskriftSteroids
Vol/bind97
Sider (fra-til)2-7
Antal sider6
ISSN0039-128X
DOI
StatusUdgivet - maj 2015

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