YC-1: A Potential Anticancer Drug Targeting Hypoxia-Inducible Factor 1 (original) (raw)

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Correspondence to: Jong-Wan Park, M.D., Ph.D., Department of Pharmacology, Seoul National University College of Medicine, 28 Yongon-dong, Chongno-gu, Seoul 110–799, Korea (e-mail: parkjw@plaza.snu.ac.kr).

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Received:

20 September 2002

Revision received:

16 January 2003

Accepted:

28 January 2003

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Eun-Jin Yeo, Yang-Sook Chun, Young-Suk Cho, Jinho Kim, June-Chul Lee, Myung-Suk Kim, Jong-Wan Park, YC-1: A Potential Anticancer Drug Targeting Hypoxia-Inducible Factor 1, JNCI: Journal of the National Cancer Institute, Volume 95, Issue 7, 2 April 2003, Pages 516–525, https://doi.org/10.1093/jnci/95.7.516
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Abstract

Background: Hypoxia-inducible factor 1 alpha (HIF-1α), a component of HIF-1, is expressed in human tumors and renders cells able to survive and grow under hypoxic (low-oxygen) conditions. YC-1, 3-(5′-hydroxymethyl-2′-furyl)-1-benzylindazole, 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 mm3, mice received daily intraperitoneal injections of vehicle or YC-1 (30 μg/g) for 2 weeks. HIF-1α protein levels and vascularity in tumors were assessed by immunohistochemistry, and the expression of HIF-1-inducible genes (vascular endothelial growth factor, aldolase, and enolase) was assessed by reverse transcription–polymerase chain reaction. All statistical tests were two-sided. Results: Compared with tumors from vehicle-treated mice, tumors from YC-1-treated mice were statistically significantly smaller (P<.01 for all comparisons), expressed lower levels of HIF-1α (P<.01 for all comparisons), were less vascularized (P<.01 for all comparisons), and expressed lower levels of HIF-1-inducible genes, regardless of tumor type. Conclusions: The inhibition of HIF-1α activity in tumors from YC-1-treated mice is associated with blocked angiogenesis and an inhibition of tumor growth. YC-1 has the potential to become the first antiangiogenic anticancer agent to target HIF-1α.

© Oxford University Press

Topic:

• angiogenesis
• polymerase chain reaction
• oxygen
• vascular endothelial growth factor a
• immunohistochemistry
• hypoxia
• antineoplastic agents
• liver neoplasms
• aldehyde-lyases
• angiogenesis inhibitors
• carcinoma, hepatocellular
• fructose-bisphosphate aldolase
• genes
• intraperitoneal injections
• natural killer cells
• enolase
• transplantation, heterologous
• mice
• neoplasms
• platelet aggregation
• liver cancer
• renal carcinoma
• tumor growth
• cervix carcinoma
• national cancer institute
• hypoxia-inducible factor 1

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