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Discovery of benzodioxane analogues as lead candidates of AIMP2-DX2 inhibitors
DC Field | Value | Language |
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dc.date.accessioned | 2023-06-02T00:48:10Z | - |
dc.date.available | 2023-06-02T00:48:10Z | - |
dc.date.issued | 2022-10 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/194450 | - |
dc.description.abstract | Aminoacyl-tRNA synthetase (ARS) interacting multifunctional protein2 (AIMP2) plays a vital role in protein synthesis. However, a splicing variant in which the second of the four exons of AIMP2 is deleted, inhibits the tumor suppression activity of AIMP2. Herein, we describe our discovery of series of potent AIMP2-DX2 inhibitors that are targeting lung cancer. Optimization of series using ligand-based drug design strategy led to discovery of compound 35, a potent AIMP2-DX2 inhibitor that is the most efficacious in H460 and A549 cells. This benzodioxane series may represent good starting points for further lead optimization of the identification potential drug candidates for the AIMP2-DX2 targeted treatment of lung cancer. | - |
dc.description.statementOfResponsibility | restriction | - |
dc.language | English | - |
dc.publisher | Pergamon Press | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.subject.MESH | A549 Cells | - |
dc.subject.MESH | Amino Acyl-tRNA Synthetases* | - |
dc.subject.MESH | Cell Line, Tumor | - |
dc.subject.MESH | Exons | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Lung Neoplasms* / pathology | - |
dc.subject.MESH | Nuclear Proteins | - |
dc.title | Discovery of benzodioxane analogues as lead candidates of AIMP2-DX2 inhibitors | - |
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 | Young Mi Kim | - |
dc.contributor.googleauthor | Sunghoon Kim | - |
dc.contributor.googleauthor | Inhee Choi | - |
dc.identifier.doi | 10.1016/j.bmcl.2022.128889 | - |
dc.relation.journalcode | J00326 | - |
dc.identifier.eissn | 1464-3405 | - |
dc.identifier.pmid | 35842206 | - |
dc.identifier.url | https://www.sciencedirect.com/science/article/pii/S0960894X22003651 | - |
dc.subject.keyword | AIMP2-DX2 | - |
dc.subject.keyword | Ligand-based drug design | - |
dc.subject.keyword | Lung cancer | - |
dc.subject.keyword | SAR | - |
dc.citation.volume | 73 | - |
dc.citation.startPage | 128889 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, Vol.73 : 128889, 2022-10 | - |
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