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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...
Autores principales: | Galdeano, Carles, Gadd, Morgan S., Soares, Pedro, Scaffidi, Salvatore, Van Molle, Inge, Birced, Ipek, Hewitt, Sarah, Dias, David M., Ciulli, Alessio |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2014
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4207132/ https://www.ncbi.nlm.nih.gov/pubmed/25166285 http://dx.doi.org/10.1021/jm5011258 |
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