Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening. Issue 87 (5th October 2016)

• Record Type: Journal Article
• Authors: Yang, Chao; Wang, Wanhe; Chen, Linmin; Liang, Jiaxin; Lin, Sheng; Lee, Ming-Yuen; Ma, Dik-Lung; Leung, Chung-Hang
• Is Part Of: Chemical communications. Volume 52:Issue 87(2016)
• Page Start: 12837
• Page End: 12840
• Publication Date: 2016-10-05
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c6cc04938a
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : We describe herein compound1, which is similar to many known natural products, as an inhibitor of the VHL–HIF1α interaction via structure-based virtual screening. Abstract : We describe herein compound1, which is similar to many known natural products, as an inhibitor of the VHL–HIF1α interaction via structure-based virtual screening. Compound1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound1 is a member of only the second class of small molecule inhibitors of the VHL–HIF1α interaction.