Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1[alpha]

By design: Novel small-molecule inhibitors of the interaction between the vonHippel-Lindau ligase (VHL) and its molecular target HIF1α, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC(50) value of 0.9μM and is thus the fi...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2012-11, Vol.51 (46), p.11463
Main Authors: Buckley, Dennis L, Gustafson, Jeffrey L, VanMolle, Inge, Roth, Anke G, Tae, Hyun Seop, Gareiss, Peter C, Jorgensen, William L, Ciulli, Alessio, Crews, Craig M
Format: Article
Language:English
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Summary:By design: Novel small-molecule inhibitors of the interaction between the vonHippel-Lindau ligase (VHL) and its molecular target HIF1α, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC(50) value of 0.9μM and is thus the first sub-micromolar inhibitor of the VHL-HIF1α interaction.
ISSN:1433-7851
1521-3773