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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...

Πλήρης περιγραφή

Αποθηκεύτηκε σε:
Λεπτομέρειες βιβλιογραφικής εγγραφής
Τόπος έκδοσης:J Med Chem
Κύριοι συγγραφείς: Soares, Pedro, Gadd, Morgan S., Frost, Julianty, Galdeano, Carles, Ellis, Lucy, Epemolu, Ola, Rocha, Sonia, Read, Kevin D., Ciulli, Alessio
Μορφή: Artigo
Γλώσσα:Inglês
Έκδοση: American Chemical Society 2017
Διαθέσιμο Online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5788404/
https://ncbi.nlm.nih.gov/pubmed/28853884
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b00675
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