TY - JOUR
T1 - Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription
AU - Féau, Clémentine
AU - Arnold, Leggy A.
AU - Kosinski, Aaron
AU - Zhu, Fangyi
AU - Connelly, Michele
AU - Guy, R. Kiplin
PY - 2009/10/16
Y1 - 2009/10/16
N2 - 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.
AB - 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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U2 - 10.1021/cb900143a
DO - 10.1021/cb900143a
M3 - Article
C2 - 19645433
AN - SCOPUS:70350153884
SN - 1554-8929
VL - 4
SP - 834
EP - 843
JO - ACS Chemical Biology
JF - ACS Chemical Biology
IS - 10
ER -