Cited 6 times in
Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact
DC Field | Value | Language |
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dc.date.accessioned | 2022-11-24T00:29:01Z | - |
dc.date.available | 2022-11-24T00:29:01Z | - |
dc.date.issued | 2021-11 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/190705 | - |
dc.description.abstract | A novel natural small molecule, voacangine (Voa), has been discovered as a potent antiangiogenic compound. Notably, Voa directly binds the kinase domain of the vascular endothelial growth factor receptor 2 (VEGFR2) and thereby inhibits downstream signaling. Herein, we developed synthetic small molecules based on the unique chemical structure of Voa that directly and specifically target and modulate the kinase activity of VEGFR2. Among these Voa structure analogues, Voa analogue 19 (V19) exhibited increased antiangiogenic potency against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects. Moreover, treatment with V19 resulted in significant tumor cell death in a mouse xenograft model. In conclusion, this new VEGFR2 modulator, inspired from the rigid scaffold of a natural compound, Voa, is presented as a potent candidate in the development of new antiangiogenic agents. | - |
dc.description.statementOfResponsibility | restriction | - |
dc.language | English | - |
dc.publisher | American Chemical Society | - |
dc.relation.isPartOf | JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.subject.MESH | Angiogenesis Inhibitors / chemistry* | - |
dc.subject.MESH | Angiogenesis Inhibitors / pharmacology* | - |
dc.subject.MESH | Animals | - |
dc.subject.MESH | Antineoplastic Agents / pharmacology | - |
dc.subject.MESH | Biological Products / chemistry | - |
dc.subject.MESH | Biological Products / pharmacology* | - |
dc.subject.MESH | Cell Death / drug effects | - |
dc.subject.MESH | Cell Line, Tumor | - |
dc.subject.MESH | Drug Development* | - |
dc.subject.MESH | Human Umbilical Vein Endothelial Cells | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Mice | - |
dc.subject.MESH | Mice, Nude | - |
dc.subject.MESH | Phosphorylation | - |
dc.subject.MESH | Structure-Activity Relationship | - |
dc.subject.MESH | Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors* | - |
dc.subject.MESH | Vascular Endothelial Growth Factor Receptor-2 / metabolism | - |
dc.subject.MESH | Xenograft Model Antitumor Assaysz | - |
dc.title | Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine (의과대학) | - |
dc.contributor.department | Dept. of Internal Medicine (내과학교실) | - |
dc.contributor.googleauthor | Sung Min Cho | - |
dc.contributor.googleauthor | Yonghyo Kim | - |
dc.contributor.googleauthor | Yooju Jung | - |
dc.contributor.googleauthor | Minjeong Ko | - |
dc.contributor.googleauthor | Gyorgy Marko-Varga | - |
dc.contributor.googleauthor | Ho Jeong Kwon | - |
dc.identifier.doi | 10.1021/acs.jmedchem.1c01168 | - |
dc.relation.journalcode | J01588 | - |
dc.identifier.eissn | 1520-4804 | - |
dc.identifier.pmid | 34730352 | - |
dc.identifier.url | https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01168 | - |
dc.citation.volume | 64 | - |
dc.citation.number | 21 | - |
dc.citation.startPage | 15858 | - |
dc.citation.endPage | 15867 | - |
dc.identifier.bibliographicCitation | JOURNAL OF MEDICINAL CHEMISTRY, Vol.64(21) : 15858-15867, 2021-11 | - |
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