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Natural products as starting materials for development of second-generation SERCA inhibitors targeted towards prostate cancer cells.

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaperJournal articleResearchpeer-review

  • Poul Nissen
  • Anne-Marie Lund Jensen, Denmark
  • Jesper Vuust Møller
  • Søren Brøgger Christensen, Pharmaceutical University of Denmark, Denmark
  • Helmer Søhoel, Pharmaceutical University of Denmark, Denmark
  • C. E. Olsen, Pharmaceutical University of Denmark, Denmark
  • S. R. Denmeade, Johns Hopkins University Hospital, United States
  • John T. Isaacs, Johns Hopkins University, United States
  • Institute of Biophysics
  • Interdisciplinary Nanoscience Center
  • Department of Molecular Biology
An analysis of the binding of the 8-O-N-tert-butoxycarbonyl-12-aminododecanoyl derivative of 8-O-debutanoylthapsigargin to the target molecule, the SERCA pump, has revealed the importance of the length and flexibility of the side chain attached to O-8. Based on the analysis a series of analogues to the 2-unsubstituted analogue trilobolide has been constructed and shown to be equipotent with thapsigargin as SERCA inhibitors. Only the 12-Boc-aminododecaonoyl derivative, however, was found to be apoptotic
Original languageEnglish
JournalBioorganic and Medicinal Chemistry
Volume14
Issue8
Pages (from-to)2810-2815
Number of pages6
Publication statusPublished - 2006

Bibliographical note

MeSH Terms:
Animals
Calcium-Transporting ATPases/antagonists & inhibitors*
Cell Line, Tumor
Humans
Male
Mass Spectrometry
Models, Molecular
Prostatic Neoplasms/enzymology
Prostatic Neoplasms/pathology*
Rabbits
Sarcoplasmic Reticulum Calcium-Transporting ATPases

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