ATP-competitive inhibitors modulate the substrate binding cooperativity of a kinase by altering its conformational entropy

ATP-competitive inhibitors are currently the largest class of clinically approved drugs for protein kinases. By targeting the ATP-binding pocket, these compounds block the catalytic activity, preventing substrate phosphorylation. A problem with these drugs, however, is that inhibited kinases may sti...

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Detalles Bibliográficos
Autores principales: Olivieri, Cristina, Li, Geoffrey C., Wang, Yingjie, V.S., Manu, Walker, Caitlin, Kim, Jonggul, Camilloni, Carlo, De Simone, Alfonso, Vendruscolo, Michele, Bernlohr, David A., Taylor, Susan S., Veglia, Gianluigi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Association for the Advancement of Science 2022
Materias:
Biomedicine and Life Sciences
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9337769/
https://www.ncbi.nlm.nih.gov/pubmed/35905186
http://dx.doi.org/10.1126/sciadv.abo0696

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