Crystal structure-guided design of bisubstrate inhibitors and photoluminiscent 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 and...

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Bibliographic Details
Main Authors: Nonga, OE, Lavogina, D, Enkvist, E, Kestav, K, Chaikuad, A, Dixon-Clarke, SE, Bullock, AN, Kopanchuk, S, Ivan, T, Ekambaram, R, Viht, K, Knapp, S, Uri, A
Format: Journal article
Language:English
Published: MDPI 2021