Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

[Image: see text] The von Hippel–Lindau tumor suppressor protein is the substrate binding subunit of the VHL E3 ubiquitin ligase, which targets hydroxylated α subunit of hypoxia inducible factors (HIFs) for ubiquitination and subsequent proteasomal degradation. VHL is a potential target for treating...

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Detalles Bibliográficos
Autores principales: Soares, Pedro, Gadd, Morgan S., Frost, Julianty, Galdeano, Carles, Ellis, Lucy, Epemolu, Ola, Rocha, Sonia, Read, Kevin D., Ciulli, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5788404/
https://www.ncbi.nlm.nih.gov/pubmed/28853884
http://dx.doi.org/10.1021/acs.jmedchem.7b00675

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5788404/
https://www.ncbi.nlm.nih.gov/pubmed/28853884
http://dx.doi.org/10.1021/acs.jmedchem.7b00675

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