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Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α.

Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM
Angew Chem Int Ed Engl 51 11463-7 (2012)
Cited: 108 times
EuropePMC logo PMID: 23065727

Abstract

E3 ubiquitin ligases, such as the therapeutically relevant VHL, are challenging targets for traditional medicinal chemistry, as their modulation requires targeting protein-protein interactions. We report novel small-molecule inhibitors of the interaction between VHL and its molecular target HIF1α, a transcription factor involved in oxygen sensing.

Reviews - 4b9k mentioned but not cited (2)

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  2. Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders. Diehl CJ, Ciulli A. Chem Soc Rev 51 8216-8257 (2022)

Articles - 4b9k mentioned but not cited (5)

  1. Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. Lucas X, Van Molle I, Ciulli A. J Med Chem 61 7387-7393 (2018)
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