Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα

[Image: see text] Covalent protein kinase inhibitors exploit currently noncatalytic cysteines in the adenosine 5′-triphosphate (ATP)-binding site via electrophiles directly appended to a reversible-inhibitor scaffold. Here, we delineate a path to target solvent-exposed cysteines at a distance >10...

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Detalles Bibliográficos
Autores principales: Borsari, Chiara, Keles, Erhan, McPhail, Jacob A., Schaefer, Alexander, Sriramaratnam, Rohitha, Goch, Wojciech, Schaefer, Thorsten, De Pascale, Martina, Bal, Wojciech, Gstaiger, Matthias, Burke, John E., Wymann, Matthias P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9011356/
https://www.ncbi.nlm.nih.gov/pubmed/35353516
http://dx.doi.org/10.1021/jacs.1c13568

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