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Effects of the potential chemopreventive agent DMU-135 on adenoma development in the ApcMin+ mouse.

Abstract
DMU-135 (3,4-Methylenedioxy-3',4',5'-trimethoxy chalcone) is a novel anticancer prodrug designed to be activated into a potent tyrosine kinase inhibitor by the tumour selective enzyme activity of the cytochrome P450 enzyme CYP1B1. CYP1B1 is selectively expressed in a wide variety of tumours including colon. The hypothesis was tested that DMU-135 would inhibit Apc(Min/+) mouse gastrointestinal adenoma formation. From 4-18 weeks of age animals received DMU-135 (0.2% w:w) in AIN93G diet. DMU-135 was well tolerated, induced no systemic side-effects and reduced adenoma multiplicity by 46 +/- 18.3% compared to controls (p < 0.001). Further characterisation of this promising chemopreventive agent is required.
AuthorsS Sale, R G Tunstall, K C Ruparelia, P C Butler, G A Potter, W P Steward, A J Gescher
JournalInvestigational new drugs (Invest New Drugs) Vol. 24 Issue 6 Pg. 459-64 (Nov 2006) ISSN: 0167-6997 [Print] United States
PMID16505954 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 3,4-methylenedioxy-3',4',5'-trimethoxy chalcone
  • Antineoplastic Agents
  • Prodrugs
  • Chalcone
  • Protein-Tyrosine Kinases
Topics
  • Adenoma (pathology, prevention & control)
  • Animals
  • Antineoplastic Agents (pharmacology, therapeutic use)
  • Chalcone (analogs & derivatives, pharmacology, therapeutic use)
  • Colon (drug effects, pathology)
  • Disease Models, Animal
  • Genes, APC
  • Hematocrit
  • Intestinal Neoplasms (pathology, prevention & control)
  • Intestine, Small (drug effects, pathology)
  • Mice
  • Mice, Inbred C57BL (genetics)
  • Prodrugs (pharmacology, therapeutic use)
  • Protein-Tyrosine Kinases (antagonists & inhibitors)

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