Literature DB >> 16505954

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

S Sale1, R G Tunstall, K C Ruparelia, P C Butler, G A Potter, W P Steward, A J Gescher.   

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.

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Year:  2006        PMID： 16505954     DOI： 10.1007/s10637-006-5947-0

Source DB:  PubMed          Journal:  Invest New Drugs        ISSN： 0167-6997            Impact factor:   3.850


  24 in total

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Authors:  Stewart Sale; Richard G Tunstall; Ketan C Ruparelia; Gerry A Potter; William P Steward; Andreas J Gescher
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