Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription. ACS Chem Biol 2009 Oct 16;4(10):834-43
Date
08/04/2009Pubmed ID
19645433Pubmed Central ID
PMC2763043DOI
10.1021/cb900143aScopus ID
2-s2.0-70350153884 (requires institutional sign-in at Scopus site) 22 CitationsAbstract
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.
Author List
Féau C, Arnold LA, Kosinski A, Zhu F, Connelly M, Guy RKAuthor
Alexander (Leggy) Arnold PhD Professor in the Chemistry & Biochemistry department at University of Wisconsin - MilwaukeeMESH terms used to index this publication - Major topics in bold
Androgen Receptor AntagonistsAntineoplastic Agents
Antineoplastic Agents, Hormonal
Cell Line, Tumor
Flufenamic Acid
Gene Expression Regulation, Neoplastic
Humans
Male
Prostatic Neoplasms
Receptors, Androgen
Structure-Activity Relationship
Tacrolimus Binding Proteins
Transcriptional Activation
