Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

[Image: see text] E3 ubiquitin ligases are attractive targets in the ubiquitin–proteasome system, however, the development of small-molecule ligands has been rewarded with limited success. The von Hippel–Lindau protein (pVHL) is the substrate recognition subunit of the VHL E3 ligase that targets HIF...

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Détails bibliographiques
Auteurs principaux: Galdeano, Carles, Gadd, Morgan S., Soares, Pedro, Scaffidi, Salvatore, Van Molle, Inge, Birced, Ipek, Hewitt, Sarah, Dias, David M., Ciulli, Alessio
Format: Artigo
Langue:Inglês
Publié: American Chemical Society 2014
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC4207132/
https://ncbi.nlm.nih.gov/pubmed/25166285
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm5011258
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