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Synthesis and discovery of the first potent proteolysis targeting chimaera (PROTAC) degrader of AIMP2-DX2 as a lung cancer drug
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dc.date.accessioned | 2024-05-31T06:18:12Z | - |
dc.date.available | 2024-05-31T06:18:12Z | - |
dc.date.issued | 2023-12 | - |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/199700 | - |
dc.description.abstract | ARS-interacting multifunctional proteins 2 (AIMP2) is known to be a powerful tumour suppressor. However, the target AIMP2-DX2, AIMP2-lacking exon 2, is often detected in many cancer patients and cells. The predominant approach for targeting AIMP-DX2 has been attempted via small molecule mediated inhibition, but due to the lack of satisfactory activity against AIMP2-DX2, new therapeutic strategies are needed to develop a novel drug for AIMP2-DX2. Here, we report the use of the PROTAC strategy that combines small-molecule AIMP2-DX2 inhibitors with selective E3-ligase ligands with optimised linkers. Consequently, candidate compound 45 was found to be a degrader of AIMP2-DX2. Together, these findings demonstrate that our PROTAC technology targeting AIMP2-DX2 would be a potential new strategy for future lung cancer treatment. | - |
dc.description.statementOfResponsibility | open | - |
dc.language | English | - |
dc.publisher | Taylor & Francis | - |
dc.relation.isPartOf | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 자유 열람제 표시기 이미지 | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.subject.MESH | Antineoplastic Agents* / pharmacology | - |
dc.subject.MESH | Cell Line, Tumor | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Lung | - |
dc.subject.MESH | Lung Neoplasms* / drug therapy | - |
dc.subject.MESH | Lung Neoplasms* / metabolism | - |
dc.subject.MESH | Nuclear Proteins / metabolism | - |
dc.subject.MESH | Proteolysis | - |
dc.title | Synthesis and discovery of the first potent proteolysis targeting chimaera (PROTAC) degrader of AIMP2-DX2 as a lung cancer drug | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | Others | - |
dc.contributor.googleauthor | BoRa Lee | - |
dc.contributor.googleauthor | Dae Gyu Kim | - |
dc.contributor.googleauthor | Aram Lee | - |
dc.contributor.googleauthor | Young Mi Kim | - |
dc.contributor.googleauthor | Lianji Cui | - |
dc.contributor.googleauthor | Sunghoon Kim | - |
dc.contributor.googleauthor | Inhee Choi | - |
dc.identifier.doi | 10.1080/14756366.2022.2135510 | - |
dc.relation.journalcode | J03586 | - |
dc.identifier.eissn | 1475-6374 | - |
dc.identifier.pmid | 36305287 | - |
dc.subject.keyword | AIMP2-DX2 | - |
dc.subject.keyword | PROTAC | - |
dc.subject.keyword | lung cancer | - |
dc.citation.volume | 38 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 51 | - |
dc.citation.endPage | 66 | - |
dc.identifier.bibliographicCitation | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 자유 열람제 표시기 이미지, Vol.38(1) : 51-66, 2023-12 | - |
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