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Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family

We performed an X-ray crystallographic study of complexes of protein kinase PIM-1 with three inhibitors comprising an adenosine mimetic moiety, a linker, and a peptide-mimetic (d-Arg)(6) fragment. Guided by the structural models, simplified chemical structures with a reduced number of polar groups a...

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Detalles Bibliográficos
Autores principales: Nonga, Olivier E., Lavogina, Darja, Enkvist, Erki, Kestav, Katrin, Chaikuad, Apirat, Dixon-Clarke, Sarah E., Bullock, Alex N., Kopanchuk, Sergei, Ivan, Taavi, Ekambaram, Ramesh, Viht, Kaido, Knapp, Stefan, Uri, Asko
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8307404/
https://www.ncbi.nlm.nih.gov/pubmed/34299628
http://dx.doi.org/10.3390/molecules26144353