A new anti-angiogenic small molecule, G0811, inhibits angiogenesis via targeting hypoxia inducible factor (HIF)-1α signal transduction

Ki Hyun Kim; Hye Jin Jung; Ho Jeong Kwon

doi:10.1016/j.bbrc.2013.10.075

A new anti-angiogenic small molecule, G0811, inhibits angiogenesis via targeting hypoxia inducible factor (HIF)-1α signal transduction

Ki Hyun Kim, Hye Jin Jung, Ho Jeong Kwon

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

Regulation of hypoxia inducible factor (HIF)-1α stabilization, which in turn contributes to adaptation of tumor cells to hypoxia has been highlighted as a promising therapeutic target in angiogenesis-related diseases. We have identified a new small molecule, G0811, as a potent angiogenesis inhibitor that targets HIF-1α signal transduction. G0811 suppressed HIF-1α stability in cancer cells and inhibited in vitro and in vivo angiogenesis, as validated by tube formation, chemoinvasion, and chorioallantoic membrane (CAM) assays. In addition, G0811 effectively decreased the expression of vascular endothelial growth factor (VEGF), which is one of target genes of HIF-1α. However, G0811 did not exhibit anti-proliferative activities or toxicity in human umbilical vein endothelial cells (HUVECs) at effective doses. These results demonstrate that G0811 could be a new angiogenesis inhibitor that acts by targeting HIF-1α signal transduction pathway.

Original language	English
Pages (from-to)	399-404
Number of pages	6
Journal	Biochemical and Biophysical Research Communications
Volume	441
Issue number	2
DOIs	https://doi.org/10.1016/j.bbrc.2013.10.075
Publication status	Published - 2013 Nov 15

Bibliographical note

Funding Information:
This work was supported by a National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP; 2009-0092964, 2009-0083522, 2010-0017984, 2012M3A9D1054520), the Center for Food and Drug Materials of Agriculture Science & Technology Development ( PJ0079772012 ), Rural Development Administration, National R&D Program, Ministry of Health & Welfare ( 0620360-1 ), and the Brain Korea 21 Project , Republic of Korea.

All Science Journal Classification (ASJC) codes

Biophysics
Biochemistry
Molecular Biology
Cell Biology

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bbrc.2013.10.075

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title = "A new anti-angiogenic small molecule, G0811, inhibits angiogenesis via targeting hypoxia inducible factor (HIF)-1α signal transduction",

abstract = "Regulation of hypoxia inducible factor (HIF)-1α stabilization, which in turn contributes to adaptation of tumor cells to hypoxia has been highlighted as a promising therapeutic target in angiogenesis-related diseases. We have identified a new small molecule, G0811, as a potent angiogenesis inhibitor that targets HIF-1α signal transduction. G0811 suppressed HIF-1α stability in cancer cells and inhibited in vitro and in vivo angiogenesis, as validated by tube formation, chemoinvasion, and chorioallantoic membrane (CAM) assays. In addition, G0811 effectively decreased the expression of vascular endothelial growth factor (VEGF), which is one of target genes of HIF-1α. However, G0811 did not exhibit anti-proliferative activities or toxicity in human umbilical vein endothelial cells (HUVECs) at effective doses. These results demonstrate that G0811 could be a new angiogenesis inhibitor that acts by targeting HIF-1α signal transduction pathway.",

author = "Kim, {Ki Hyun} and Jung, {Hye Jin} and Kwon, {Ho Jeong}",

note = "Funding Information: This work was supported by a National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP; 2009-0092964, 2009-0083522, 2010-0017984, 2012M3A9D1054520), the Center for Food and Drug Materials of Agriculture Science & Technology Development ( PJ0079772012 ), Rural Development Administration, National R&D Program, Ministry of Health & Welfare ( 0620360-1 ), and the Brain Korea 21 Project , Republic of Korea.",

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A new anti-angiogenic small molecule, G0811, inhibits angiogenesis via targeting hypoxia inducible factor (HIF)-1α signal transduction

Abstract

Bibliographical note

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UN SDGs

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