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Small-molecules that covalently react with a human prolyl hydroxylase – towards activity modulation and substrate capture

We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2 substrates. Reversible active site binding of electrophile bearing compounds enables susbsequent covalent reaction with a lysine residue (K408...

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Detalles Bibliográficos
Autores principales: Bush, Jacob T., Leśniak, Robert K., Yeh, Tzu-Lan, Belle, Roman, Kramer, Holger, Tumber, Anthony, Chowdhury, Rasheduzzaman, Flashman, Emily, Mecinović, Jasmin, Schofield, Christopher J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6350621/
https://www.ncbi.nlm.nih.gov/pubmed/30452037
http://dx.doi.org/10.1039/c8cc07706a