Novel anti-prostate cancer curcumin analogues that enhance androgen receptor degradation activity.

Abstract:

:The androgen receptor (AR) plays a crucial role in the physiological and pathological functions of androgen. As a transcription factor, the AR modulates androgen activity by regulating the transcription of target genes that are involved in numerous physiological functions and pathological disorders, such as acne vulgaris, androgenetic alopecia, benign prostate hyperplasia (BPH), and prostate cancers. Although many natural and synthetic curcumin analogues have been reported to possess anticancer activity through a common cytotoxic property against proliferating tumor cells, none has been reported to inhibit cancer cell growth through a more specific mechanism or target in the cancer cells. Recently, new curcumin analogues were studied extensively regarding their synthesis, structure-activity (i.e., anticancer activity) relationships, and mechanism of action. These compounds, such as ASC-J9 and its analogues (3 and 4), have now been shown to inhibit prostate cancer proliferation through a novel mechanism of enhancing AR degradation.

authors

Shi Q,Shih CC,Lee KH

doi

10.2174/187152009789124655

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

904-12

issue

8

eissn

1871-5206

issn

1875-5992

pii

ACA-MC-16

journal_volume

9

pub_type

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