A-loop interactions in Mer tyrosine kinase give rise to inhibitors with two-step mechanism and long residence time of binding

The activation loop (A-loop) plays a key role in regulating the catalytic activity of protein kinases. Phosphorylation in this region enhances the phosphoryl transfer rate of the kinase domain and increases its affinity for ATP. Furthermore, the A-loop possesses autoinhibitory functions in some kina...

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Detalles Bibliográficos
Autores principales: Pflug, Alexander, Schimpl, Marianne, Nissink, J. Willem M., Overman, Ross C., Rawlins, Philip B., Truman, Caroline, Underwood, Elizabeth, Warwicker, Juli, Winter-Holt, Jon, McCoull, William
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Portland Press Ltd. 2020
Materias:
Structural Biology
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7702301/
https://www.ncbi.nlm.nih.gov/pubmed/33119085
http://dx.doi.org/10.1042/BCJ20200735

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