Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription

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

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

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.

Original languageEnglish
Pages (from-to)834-843
Number of pages10
JournalACS Chemical Biology
Volume4
Issue number10
DOIs
StatePublished - Oct 16 2009

Funding

FundersFunder number
National Institute of Diabetes and Digestive and Kidney DiseasesR55DK058080

    ASJC Scopus subject areas

    • Biochemistry
    • Molecular Medicine

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