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Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact

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dc.date.accessioned2022-11-24T00:29:01Z-
dc.date.available2022-11-24T00:29:01Z-
dc.date.issued2021-11-
dc.identifier.issn0022-2623-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/190705-
dc.description.abstractA 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.statementOfResponsibilityrestriction-
dc.languageEnglish-
dc.publisherAmerican Chemical Society-
dc.relation.isPartOfJOURNAL OF MEDICINAL CHEMISTRY-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.subject.MESHAngiogenesis Inhibitors / chemistry*-
dc.subject.MESHAngiogenesis Inhibitors / pharmacology*-
dc.subject.MESHAnimals-
dc.subject.MESHAntineoplastic Agents / pharmacology-
dc.subject.MESHBiological Products / chemistry-
dc.subject.MESHBiological Products / pharmacology*-
dc.subject.MESHCell Death / drug effects-
dc.subject.MESHCell Line, Tumor-
dc.subject.MESHDrug Development*-
dc.subject.MESHHuman Umbilical Vein Endothelial Cells-
dc.subject.MESHHumans-
dc.subject.MESHMice-
dc.subject.MESHMice, Nude-
dc.subject.MESHPhosphorylation-
dc.subject.MESHStructure-Activity Relationship-
dc.subject.MESHVascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*-
dc.subject.MESHVascular Endothelial Growth Factor Receptor-2 / metabolism-
dc.subject.MESHXenograft Model Antitumor Assaysz-
dc.titleDevelopment of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine (의과대학)-
dc.contributor.departmentDept. of Internal Medicine (내과학교실)-
dc.contributor.googleauthorSung Min Cho-
dc.contributor.googleauthorYonghyo Kim-
dc.contributor.googleauthorYooju Jung-
dc.contributor.googleauthorMinjeong Ko-
dc.contributor.googleauthorGyorgy Marko-Varga-
dc.contributor.googleauthorHo Jeong Kwon-
dc.identifier.doi10.1021/acs.jmedchem.1c01168-
dc.relation.journalcodeJ01588-
dc.identifier.eissn1520-4804-
dc.identifier.pmid34730352-
dc.identifier.urlhttps://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01168-
dc.citation.volume64-
dc.citation.number21-
dc.citation.startPage15858-
dc.citation.endPage15867-
dc.identifier.bibliographicCitationJOURNAL OF MEDICINAL CHEMISTRY, Vol.64(21) : 15858-15867, 2021-11-
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers

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