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Antischistosomal versus antiandrogenic properties of aryl hydantoin Ro 13-3978

Wang, Chunkai and Zhao, Qingjie and Min, Jaeki and Muniyan, Sakthivel and Vargas, Mireille and Wang, Xiaofang and Dong, Yuxiang and Guy, R. Kiplin and Lin, Ming-Fong and Keiser, Jennifer and Vennerstrom, Jonathan L.. (2014) Antischistosomal versus antiandrogenic properties of aryl hydantoin Ro 13-3978. American journal of tropical medicine and hygiene, Vol. 90, H. 6. pp. 1156-1158.

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Official URL: http://edoc.unibas.ch/dok/A6288970

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Abstract

In the early 1980s, the antischistosomal aryl hydantoin Ro 13-3978 (AH01), a close structural analogue of the androgen receptor antagonist nilutamide, was discovered. Administration of 100 mg/kg oral doses of AH01 to mice infected with adult and juvenile Schistosoma mansoni produced 95% and 64% total worm burden reductions, confirming its high activity against adult worms, and showing that AH01 is also effective against juvenile infections. AH01 had no measureable interaction with the androgen receptor in a ligand competition assay, but it did block dihydrotestosterone-induced cell proliferation in an androgen-dependent human prostate cancer cell line. For AH01, nilutamide, and three closely related aryl hydantoin derivatives, there was no correlation between antischistosomal activity and androgen receptor interaction.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Helminth Drug Development (Keiser)
UniBasel Contributors:Vargas, Mireille and Keiser, Jennifer
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Williams and Wilkins
ISSN:0002-9637
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:07 Nov 2014 08:28
Deposited On:07 Nov 2014 08:28

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