https://scholars.lib.ntu.edu.tw/handle/123456789/564858
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.author | Pan S.-L. | en_US |
dc.contributor.author | JIH-HWA GUH | en_US |
dc.contributor.author | Peng C.-Y. | en_US |
dc.contributor.author | Wang S.-W. | en_US |
dc.contributor.author | Chang Y.-L. | en_US |
dc.contributor.author | Cheng F.-C. | en_US |
dc.contributor.author | Chang J.-H. | en_US |
dc.contributor.author | Kuo S.-C. | en_US |
dc.contributor.author | Lee F.-Y. | en_US |
dc.contributor.author | Teng C.-M. | en_US |
dc.date.accessioned | 2021-06-02T05:44:03Z | - |
dc.date.available | 2021-06-02T05:44:03Z | - |
dc.date.issued | 2005 | - |
dc.identifier.issn | 223565 | - |
dc.identifier.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-23044433522&doi=10.1124%2fjpet.105.085126&partnerID=40&md5=c9197c090b22c56df4ea5007c9dce6f7 | - |
dc.identifier.uri | https://scholars.lib.ntu.edu.tw/handle/123456789/564858 | - |
dc.description.abstract | Angiogenesis is a process that involves endothelial cell proliferation, migration, invasion, and tube formation, and inhibition of these processes has implications for angiogenesis-mediated disorders. The purpose of this study was to evaluate the antiangiogenic efficacy of YC-1 [3-(5′-hydroxymethyl- 2′-furyl)-1-benzyl indazole] in well characterized in vitro and in vivo systems. YC-1 inhibited the ability of vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF) in a dose-dependent manner to induce proliferation, migration, and tube formation in human umbilical vascular endothelial cells; these outcomes were evaluated using [3H]thymidine incorporation, transwell chamber, and Matrigel-coated slide assays, respectively. YC-1 inhibited VEGF- and bFGF-induced p42/p44 mitogen-activated protein kinase and Akt phosphorylation as well as protein kinase Cα translocation using Western blot analysis. The effect of YC-1 on angiogenesis in vivo was evaluated using the mouse Matrigel implant model. YC-1 administered orally in doses of 1 to 100 mg/kg/day inhibited VEGF- and bFGF-induced neovascularization in a dose-dependent manner over 7 days. These results indicate that YC-1 has antiangiogenic activity at very low doses. Moreover, in transplantable murine tumor models, YC-1 administered orally displayed a high degree of antitumor activity (treatment-to-control life span ratio > 175%) without cytotoxicity. YC-1 may be useful for treating angiogenesis-dependent human diseases such as cancer. Copyright ? 2005 by The American Society for Pharmacology and Experimental Therapeutics. | - |
dc.relation.ispartof | Journal of Pharmacology and Experimental Therapeutics | - |
dc.subject.classification | [SDGs]SDG3 | - |
dc.subject.other | 1 benzyl 3 (5 hydroxymethyl 2 furyl)indazole; angiogenic factor; basic fibroblast growth factor; matrigel; mitogen activated protein kinase 1; mitogen activated protein kinase 3; protein kinase B; protein kinase C alpha; tritium; vasculotropin; angiogenesis; animal experiment; animal model; antiangiogenic activity; antineoplastic activity; article; bioassay; cancer therapy; cell function; cell migration; cell proliferation; controlled study; cytotoxicity; DNA synthesis; dose response; endometrium cell; human; human cell; lifespan; low drug dose; mouse; neovascularization (pathology); nonhuman; priority journal; protein phosphorylation; protein transport; tumor model; Western blotting; 1-Phosphatidylinositol 3-Kinase; Angiogenesis Inducing Agents; Angiogenesis Inhibitors; Blotting, Western; Cell Movement; Cell Proliferation; Endothelial Cells; Endothelium, Vascular; Enzyme Activators; Extracellular Signal-Regulated MAP Kinases; Fibroblast Growth Factor 2; Guanylate Cyclase; Humans; Indazoles; Longevity; Microtubules; Neoplasms; Neovascularization, Pathologic; Protein Kinase C; Signal Transduction; Tetrazolium Salts; Thiazoles; Thymidine; Vascular Endothelial Growth Factor A | - |
dc.title | YC-1 [3-(5′-hydroxymethyl-2′-furyl)-1-benzyl indazole] inhibits endothelial cell functions induced by angiogenic factors in vitro and angiogenesis in vivo models | en_US |
dc.type | journal article | en |
dc.identifier.doi | 10.1124/jpet.105.085126 | - |
dc.identifier.pmid | 15784655 | - |
dc.identifier.scopus | 2-s2.0-23044433522 | - |
dc.relation.pages | 35-42 | - |
dc.relation.journalvolume | 314 | - |
dc.relation.journalissue | 1 | - |
item.openairetype | journal article | - |
item.openairecristype | http://purl.org/coar/resource_type/c_6501 | - |
item.cerifentitytype | Publications | - |
item.fulltext | no fulltext | - |
item.grantfulltext | none | - |
crisitem.author.dept | Pharmacy | - |
crisitem.author.dept | School of Pharmacy | - |
crisitem.author.orcid | 0000-0002-6738-6054 | - |
crisitem.author.parentorg | College of Medicine | - |
crisitem.author.parentorg | College of Medicine | - |
顯示於: | 藥學系 |
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