Issue 87, 2016

Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

Abstract

We describe herein compound 1, which is similar to many known natural products, as an inhibitor of the VHL–HIF1α interaction via structure-based virtual screening. Compound 1 disrupts VHL-mediated HIF1α degradation, leading to significantly increased VEGF expression. To our knowledge, compound 1 is a member of only the second class of small molecule inhibitors of the VHL–HIF1α interaction.

Graphical abstract: Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

Supplementary files

Article information

Article type
Communication
Submitted
13 Jun 2016
Accepted
27 Sep 2016
First published
05 Oct 2016

Chem. Commun., 2016,52, 12837-12840

Discovery of a VHL and HIF1α interaction inhibitor with in vivo angiogenic activity via structure-based virtual screening

C. Yang, W. Wang, L. Chen, J. Liang, S. Lin, M. Lee, D. Ma and C. Leung, Chem. Commun., 2016, 52, 12837 DOI: 10.1039/C6CC04938A

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements