Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells
DC Field | Value | Language |
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dc.contributor.author | Ryu, Byung Jun | - |
dc.contributor.author | Baek, Seung-hwa | - |
dc.contributor.author | Kim, Jiyeon | - |
dc.contributor.author | Bae, Su Jung | - |
dc.contributor.author | Chang, Sung-Youn | - |
dc.contributor.author | Heo, Jung-Nyoung | - |
dc.contributor.author | Lee, Hyuk | - |
dc.contributor.author | Lee, Sang Yeol | - |
dc.contributor.author | Kim, Seong Hwan | - |
dc.date.available | 2020-02-29T05:43:22Z | - |
dc.date.created | 2020-02-06 | - |
dc.date.issued | 2012-09-01 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/16170 | - |
dc.description.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. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.subject | PROTEIN-KINASE CK2 | - |
dc.subject | ANDROGEN RECEPTOR | - |
dc.subject | GENE-EXPRESSION | - |
dc.subject | PROLIFERATION | - |
dc.subject | MECHANISMS | - |
dc.subject | CK2-ALPHA | - |
dc.subject | INTERACTS | - |
dc.subject | CX-4945 | - |
dc.title | Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells | - |
dc.type | Article | - |
dc.type.rims | ART | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000308046400023 | - |
dc.identifier.doi | 10.1016/j.bmcl.2012.07.031 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.17, pp.5470 - 5474 | - |
dc.identifier.scopusid | 2-s2.0-84865135592 | - |
dc.citation.endPage | 5474 | - |
dc.citation.startPage | 5470 | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 22 | - |
dc.citation.number | 17 | - |
dc.contributor.affiliatedAuthor | Lee, Sang Yeol | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | CK2 | - |
dc.subject.keywordAuthor | CX4945 | - |
dc.subject.keywordAuthor | Androgen receptor | - |
dc.subject.keywordAuthor | Apoptosis | - |
dc.subject.keywordAuthor | Prostate cancer | - |
dc.subject.keywordPlus | PROTEIN-KINASE CK2 | - |
dc.subject.keywordPlus | ANDROGEN RECEPTOR | - |
dc.subject.keywordPlus | GENE-EXPRESSION | - |
dc.subject.keywordPlus | PROLIFERATION | - |
dc.subject.keywordPlus | MECHANISMS | - |
dc.subject.keywordPlus | CK2-ALPHA | - |
dc.subject.keywordPlus | INTERACTS | - |
dc.subject.keywordPlus | CX-4945 | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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