Full metadata record

DC Field Value Language
dc.contributor.authorSeo, Myeong-Seong-
dc.contributor.authorJung, Kyung Hee-
dc.contributor.authorKim, Kewon-
dc.contributor.authorLee, Ji Eun-
dc.contributor.authorHan, Beom Seok-
dc.contributor.authorKo, Soyeon-
dc.contributor.authorKIM, JAE HO-
dc.contributor.authorHong, Sungwoo-
dc.contributor.authorLee, So Ha-
dc.contributor.authorHong, Soon-Sun-
dc.date.accessioned2024-01-12T03:01:13Z-
dc.date.available2024-01-12T03:01:13Z-
dc.date.created2022-06-17-
dc.date.issued2022-08-
dc.identifier.issn0753-3322-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/76655-
dc.description.abstractThe novel (nua) kinase family 1 (NUAK1) is an AMPK-related kinase and its expression is associated with tumor malignancy and poor prognosis in several types of cancer, suggesting its potential as a target for cancer therapy. Therefore, the development of NUAK1-targeting inhibitors could improve therapeutic outcomes in cancer. We synthesized KI-301670, a novel NUAK1 inhibitor, and assessed its anticancer effects and mechanism of action in pancreatic cancer. It effectively inhibited pancreatic cancer growth and proliferation, and induced cell cycle arrest, markedly G0/G1 arrest, by increasing the expression of p27 and decreasing expression of p-Rb and E2F1. Additionally, the apoptotic effect of KI-301670 was observed by an increase in cleaved PARP, TUNEL-positive cells, and annexin V cell population, as well as the release of cytochrome c via the loss of mitochondrial membrane potential. KI-301670 inhibited the migration and invasion of pancreatic cancer cells. Mechanistically, KI-301670 effectively inhibited the PI3K/AKT pathway in pancreatic cancer cells. Furthermore, it significantly attenuated tumor growth in a mouse xenograft tumor model. Our results demonstrate that a novel NUAK1 inhibitor, KI-301670, exerts anti-tumor effects by directly suppressing cancer cell growth by affecting the PI3K/ AKT pathway, suggesting that it could be a novel therapeutic candidate for pancreatic cancer treatment.-
dc.languageEnglish-
dc.publisherElsevier Masson-
dc.titleDiscovery of a novel NUAK1 inhibitor against pancreatic cancer-
dc.typeArticle-
dc.identifier.doi10.1016/j.biopha.2022.113241-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBiomedicine and Pharmacotherapy, v.152-
dc.citation.titleBiomedicine and Pharmacotherapy-
dc.citation.volume152-
dc.description.isOpenAccessY-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000815801200005-
dc.relation.journalWebOfScienceCategoryMedicine, Research & Experimental-
dc.relation.journalWebOfScienceCategoryPharmacology & Pharmacy-
dc.relation.journalResearchAreaResearch & Experimental Medicine-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.type.docTypeArticle-
dc.subject.keywordPlusEPITHELIAL-MESENCHYMAL TRANSITION-
dc.subject.keywordPlusPI3K/AKT SIGNALING PATHWAY-
dc.subject.keywordPlusARK5-
dc.subject.keywordPlusEXPRESSION-
dc.subject.keywordPlusAMPK-
dc.subject.keywordPlusMETASTASIS-
dc.subject.keywordPlusRESISTANCE-
dc.subject.keywordPlusCELLS-
dc.subject.keywordPlusCARCINOMA-
dc.subject.keywordPlusINVASION-
dc.subject.keywordAuthorApoptosis-
dc.subject.keywordAuthorNUAK1-
dc.subject.keywordAuthorKI-301670-
dc.subject.keywordAuthorPancreatic cancer-
dc.subject.keywordAuthorPI3K-
dc.subject.keywordAuthorAKT pathway-
Appears in Collections:
KIST Article > 2022
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML

qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE