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Nucleotide based covalent inhibitors of KRas can only be efficient in vivo if they bind reversibly with GTP-like affinity

Simple reversible competitive inhibition of nucleotide binding of GTP to Ras family GTPases has long been recognized as an unlikely approach to manipulating the activity of such proteins for experimental or therapeutic purposes. This is due to the high affinity of GTP to GTPases coupled with high ce...

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Detalles Bibliográficos
Autores principales: Müller, Matthias P., Jeganathan, Sadasivam, Heidrich, Angelika, Campos, Jeremy, Goody, Roger S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5473928/
https://www.ncbi.nlm.nih.gov/pubmed/28623374
http://dx.doi.org/10.1038/s41598-017-03973-6