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ARTICLES YC-1: A Potential Anticancer Drug Targeting Hypoxia-Inducible Factor 1

By Eun-jin Yeo, Yang-sook Chun, Young-suk Cho, Jinho Kim, June-chul Lee, Myung-suk Kim and Jong-wan Park


component of HIF-1, is expressed in human tumors and renders cells able to survive and grow under hypoxic (lowoxygen) conditions. YC-1, 3-(5�-hydroxymethyl-2�-furyl)-1benzylindazole, an agent developed for circulatory disorders that inhibits platelet aggregation and vascular contraction, inhibits HIF-1 activity in vitro. We tested whether YC-1 inhibits HIF-1 and tumor growth in vivo. Methods: Hep3B hepatoma, NCI-H87 stomach carcinoma, Caki-1 renal carcinoma, SiHa cervical carcinoma, and SK-N-MC neuroblastoma cells were grown as xenografts in immunodeficient mice (69 mice total). After the tumors were 100–150 mm 3, mice received daily intraperitoneal injections of vehicle or YC-1 (30 µg/g) for 2 weeks. HIF-1 � protein levels and vascularity in tumors were assessed by immunohistochemistry, and the expression of HIF-1-inducible genes (vascular endothelia

Year: 2013
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