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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.