Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Javascript disabled

Please enable Javascript support in your browser to use this application.

Instructions on how to enable JavaScript on different browsers can be found here: http://www.google.com/support/bin/answer.py?answer=23852.

[edit this page]

Chemical Compound Review:

R-85246 but-2-enedioic acid; 6-[(3-chlorophenyl)...

Synonyms: AC1O5L67, 145858-52-2, UNII-91W7VLK7J3, 115575-11-6 (Parent)

This record was replaced with 60652.

Wan, X.S. et al., Van heusden, J. et al., Goss, P.E. et al., Ly, L.H. et al., Van Wauwe, J. et al.

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of R-75251

To examine this hypothesis we explored combination therapy with liarozole fumarate (R85,246), an imidazole derivative currently in trials for prostate cancer therapy [1].

High impact information on R-75251

Liarozole-fumarate is an anti-tumour drug that inhibits the cytochrome P450-dependent catabolism of ATRA [2].
Liarozole-fumarate alone up to a concentration of 10(-6) M had no effect on MCF-7 cell proliferation [2].
The inhibitory effect of liarozole fumarate on this metabolic process may contribute to the reported retinoid-mimetic activity of this drug [3].
Three phase II studies were conducted to determine the efficacy and tolerability of liarozole fumarate (R85246; liarozole), a retinoic acid metabolism blocking agent (RAMBA) and aromatase inhibitor [4].
9-cis retinoic acid, genistein, liarozole fumarate, p-XSC, L-selenomethionine and vitamin E also showed much stronger growth inhibitory effects on BRF-55T cells than on the normal prostate epithelial cells, indicating that these agents may also be useful for the prevention and treatment of BPH [5].

References

Liarozole acts synergistically with 1alpha,25-dihydroxyvitamin D3 to inhibit growth of DU 145 human prostate cancer cells by blocking 24-hydroxylase activity. Ly, L.H., Zhao, X.Y., Holloway, L., Feldman, D. Endocrinology (1999) [Pubmed]
The antiproliferative activity of all-trans-retinoic acid catabolites and isomers is differentially modulated by liarozole-fumarate in MCF-7 human breast cancer cells. Van heusden, J., Wouters, W., Ramaekers, F.C., Krekels, M.D., Dillen, L., Borgers, M., Smets, G. Br. J. Cancer (1998) [Pubmed]
Liarozole fumarate inhibits the metabolism of 4-keto-all-trans-retinoic acid. Van Wauwe, J., Coene, M.C., Cools, W., Goossens, J., Lauwers, W., Le Jeune, L., Van Hove, C., Van Nyen, G. Biochem. Pharmacol. (1994) [Pubmed]
Liarozole fumarate (R85246): in the treatment of ER negative, tamoxifen refractory or chemotherapy resistant postmenopausal metastatic breast cancer. Goss, P.E., Strasser, K., Marques, R., Clemons, M., Oza, A., Goel, R., Blackstein, M., Kaizer, L., Sterns, E.E., Nabholtz, J.M., De Coster, R., Crump, M., Abdolell, M., Qi, S. Breast Cancer Res. Treat. (2000) [Pubmed]
In vitro evaluation of chemopreventive agents using cultured human prostate epithelial cells. Wan, X.S., Zhou, Z., Kennedy, A.R., Kopelovich, L. Oncol. Rep. (2003) [Pubmed]

Contributions to this collaborative article are from individual authors of WikiGenes or mined by the WikiGenes Data Mining Engine from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.About WikiGenes Open Access Licence Privacy Policy Terms of Use

[search][advanced]