Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α | Zendy

Buckley Dennis L. | Zendy; Gustafson Jeffrey L. | Zendy; Van Molle Inge | Zendy; Roth Anke G. | Zendy; Tae Hyun Seop | Zendy; Gareiss Peter C. | Zendy; Jorgensen William L. | Zendy; Ciulli Alessio | Zendy; Crews Craig M. | Zendy

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Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

Author(s) -

Buckley Dennis L.,

Gustafson Jeffrey L.,

Van Molle Inge,

Roth Anke G.,

Tae Hyun Seop,

Gareiss Peter C.,

Jorgensen William L.,

Ciulli Alessio,

Crews Craig M.

Publication year - 2012

Publication title -

angewandte chemie international edition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.201206231

Subject(s) - dna ligase , small molecule , ubiquitin ligase , computational biology , computer science , ic50 , transcription (linguistics) , chemistry , biochemistry , information retrieval , bioinformatics , biology , enzyme , gene , in vitro , ubiquitin , philosophy , linguistics

By design : Novel small‐molecule inhibitors of the interaction between the von Hippel–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 0.9 μ M and is thus the first sub‐micromolar inhibitor of the VHL–HIF1α interaction.

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