Literature DB >> 19645433

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.

Clémentine Féau1, Leggy A Arnold, Aaron Kosinski, Fangyi Zhu, Michele Connelly, R Kiplin Guy.   

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.

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Year:  2009        PMID： 19645433      PMCID： PMC2763043          DOI： 10.1021/cb900143a

Source DB:  PubMed          Journal:  ACS Chem Biol        ISSN： 1554-8929            Impact factor:   5.100


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