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Anti-cancer effect of novel PAK1 inhibitor via induction of PUMA-mediated cell death and p21-mediated cell cycle arrest
DC Field | Value | Language |
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dc.contributor.author | Woo, Tae-Gyun | - |
dc.contributor.author | Yoon, Min-Ho | - |
dc.contributor.author | Hong, Shin-Deok | - |
dc.contributor.author | Choi, Jiyun | - |
dc.contributor.author | Ha, Nam-Chul | - |
dc.contributor.author | Sun, Hokeun | - |
dc.contributor.author | Park, Bum-Joon | - |
dc.creator | 하남출 | - |
dc.date.accessioned | 2019-04-24T08:29:47Z | - |
dc.date.available | 2020-04-05T08:29:47Z | - |
dc.date.created | 2018-01-10 | - |
dc.date.issued | 2017-04 | - |
dc.identifier.citation | Oncotarget, Vol.8 No.14, pp.23690-23701 | - |
dc.identifier.issn | 1949-2553 | - |
dc.identifier.uri | https://hdl.handle.net/10371/147880 | - |
dc.description.abstract | Hyper-activation of PAK1 (p21-activated kinase 1) is frequently observed in human cancer and speculated as a target of novel anti-tumor drug. In previous, we also showed that PAK1 is highly activated in the Smad4-deficient condition and suppresses PUMA (p53 upregulated modulator of apoptosis) through direct binding and phosphorylation. On the basis of this result, we have tried to find novel PAK1-PUMA binding inhibitors. Through ELISA-based blind chemical library screening, we isolated single compound, IPP-14 (IPP; Inhibitor of PAK1-PUMA), which selectively blocks the PAK1-PUMA binding and also suppresses cell proliferation via PUMAdependent manner. Indeed, in PUMA-deficient cells, this chemical did not show anti-proliferating effect. This chemical possessed very strong PAK1 inhibition activity that it suppressed BAD (Bcl-2-asoociated death promoter) phosphorylation and meta-phase arrest via Aurora kinase inactivation in lower concentration than that of previous PAK1 kinase, FRAX486 and AG879. Moreover, our chemical obviously induced p21/WAF1/CIP1 (Cyclin-dependent kinase inhibitor 1A) expression by releasing from Bcl-2 (B-cell lymphoma-2) and by inhibition of AKT-mediated p21 suppression. Considering our result, IPP-14 and its derivatives would be possible candidates for PAK1 and p21 induction targeted anti-cancer drug. | - |
dc.language | 영어 | - |
dc.language.iso | en | en |
dc.publisher | Impact Journals | - |
dc.title | Anti-cancer effect of novel PAK1 inhibitor via induction of PUMA-mediated cell death and p21-mediated cell cycle arrest | - |
dc.type | Article | - |
dc.identifier.doi | 10.18632/oncotarget.15783 | - |
dc.citation.journaltitle | Oncotarget | - |
dc.identifier.wosid | 000398211100117 | - |
dc.identifier.scopusid | 2-s2.0-85016926428 | - |
dc.description.srnd | OAIID:RECH_ACHV_DSTSH_NO:T201716382 | - |
dc.description.srnd | RECH_ACHV_FG:RR00200001 | - |
dc.description.srnd | ADJUST_YN: | - |
dc.description.srnd | EMP_ID:A079611 | - |
dc.description.srnd | CITE_RATE:5.168 | - |
dc.description.srnd | FILENAME:oncotarget_PUMA_2017.pdf | - |
dc.description.srnd | DEPT_NM:농생명공학부 | - |
dc.description.srnd | EMAIL:hanc210@snu.ac.kr | - |
dc.description.srnd | SCOPUS_YN:Y | - |
dc.description.srnd | FILEURL:https://srnd.snu.ac.kr/eXrepEIR/fws/file/150145fa-97e8-45fa-8271-e8068f58c661/link | - |
dc.citation.endpage | 23701 | - |
dc.citation.number | 14 | - |
dc.citation.startpage | 23690 | - |
dc.citation.volume | 8 | - |
dc.description.isOpenAccess | Y | - |
dc.contributor.affiliatedAuthor | Ha, Nam-Chul | - |
dc.identifier.srnd | T201716382 | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | TUMOR-SUPPRESSOR GENE | - |
dc.subject.keywordPlus | CANCER-CELLS | - |
dc.subject.keywordPlus | P21-ACTIVATED KINASES | - |
dc.subject.keywordPlus | APOPTOTIC RESPONSE | - |
dc.subject.keywordPlus | AURORA-A | - |
dc.subject.keywordPlus | P53 | - |
dc.subject.keywordPlus | ACTIVATION | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | PHOSPHORYLATION | - |
dc.subject.keywordPlus | LOCALIZATION | - |
dc.subject.keywordAuthor | PAK1 | - |
dc.subject.keywordAuthor | anti-cancer | - |
dc.subject.keywordAuthor | p21 | - |
dc.subject.keywordAuthor | PUMA | - |
dc.subject.keywordAuthor | Bcl-2 | - |
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