Novel Anti-Prostate Cancer Curcumin Analogues That Enhance Androgen Receptor Degradation Activity

Author(s): Q. Shi, C. C.-Y. Shih, K. H. Lee

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 9 , Issue 8 , 2009

Become EABM
Become Reviewer
Call for Editor


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.

Keywords: Androgen receptor (AR), Curcumin analogues, Anti-prostate cancer activity, AR degradation

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2009
Published on: 01 March, 2012
Page: [904 - 912]
Pages: 9
DOI: 10.2174/187152009789124655
Price: $65

Article Metrics

PDF: 26