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Updated: Jun 21, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription
Clémentine Féau1, Leggy A Arnold, Aaron Kosinski
1Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, USA.
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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