Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells
- Authors
- Ryu, Byung Jun; Baek, Seung-hwa; Kim, Jiyeon; Bae, Su Jung; Chang, Sung-Youn; Heo, Jung-Nyoung; Lee, Hyuk; Lee, Sang Yeol; Kim, Seong Hwan
- Issue Date
- 1-Sep-2012
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- CK2; CX4945; Androgen receptor; Apoptosis; Prostate cancer
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.17, pp.5470 - 5474
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 22
- Number
- 17
- Start Page
- 5470
- End Page
- 5474
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/16170
- DOI
- 10.1016/j.bmcl.2012.07.031
- ISSN
- 0960-894X
- Abstract
- Androgen receptor (AR) is crucial for transcriptional signaling in prostate cancers. The anti-cancer activity of protein kinase CK2 (formerly called casein kinase 2)-specific small molecule inhibitors have been reported in several cancers including prostate cancers. The orally available CX4945, a potent and selective small molecule inhibitor of CK2, has advanced into human clinical trials and has exhibited strong antitumor activity. The inhibition of CK2 leads to a down-regulation of the AR-dependent transcription, but the functional relevance of CX4945 to AR-dependent transcription in AR-positive LNCap cells has not been studied yet. Our observation of inhibitory effects of CX4945 on the expression or phosphorylation levels of CK2 alpha, Akt and anti-apoptotic molecules including IAP family members agreed with a previous study showing the effect of CK2 inhibition in cancer cells. This study also provides novel information on the impact of CX4945 in the inhibition of AR-dependent transcriptional activation in LNCap cells via its down-regulation. Pharmacologic inhibition experiment revealed that CX4945 could exhibit its anti-cancer activity in LNCap cells via the independent inhibitions of AR and Akt-survivin signalings. (C) 2012 Elsevier Ltd. All rights reserved.
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