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American Chemical Society, ACS Chemical Biology, 10(4), p. 834-843, 2009

DOI: 10.1021/cb900143a

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Novel Flufenamic Acid Analogues as Inhibitors of Androgen Receptor Mediated Transcription

Journal article published in 2009 by Clémentine Féau, Leggy A. Arnold, Aaron Kosinski, Fangyi Zhu, Michele Connelly, R. Kiplin Guy ORCID
This paper is available in a repository.
This paper is available in a repository.

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Abstract

The androgen receptor (AR), which mediates the signals of androgens, plays a crucial role in prostate-related diseases. Although widely used, currently marketed anti-androgenic drugs have significant side effects. Several studies have revealed that non-steroidal anti-inflammatory drugs, such as flufenamic acid, block AR transcriptional activity. Herein we describe the development of small molecule analogues of flufenamic acid that antagonize AR. This novel class of AR inhibitors binds to the hormone binding site, blocks AR transcription activity, and acts on AR target genes.