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

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 (<span style="font-variant: small-caps;">d</span>-Arg)<sub>6</sub> fragment. Guided by the...

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Bibliographic Details
Main Authors: Olivier E. Nonga, Darja Lavogina, Erki Enkvist, Katrin Kestav, Apirat Chaikuad, Sarah E. Dixon-Clarke, Alex N. Bullock, Sergei Kopanchuk, Taavi Ivan, Ramesh Ekambaram, Kaido Viht, Stefan Knapp, Asko Uri
Format: Article
Language:English
Published: MDPI AG 2021-07-01
Series:Molecules
Subjects:
protein X-ray crystallography
co-crystal structure
PIM kinases
bisubstrate inhibitors
fluorescent probes
cellular uptake and localization
Online Access:https://www.mdpi.com/1420-3049/26/14/4353

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https://www.mdpi.com/1420-3049/26/14/4353

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