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Potent and selective: The unique nature of the ATP binding pocket structure of Pim family protein kinases (PKs) was used for the development of bisubstrate inhibitors and a fluorescent probe with sub-nanomolar affinity. Conjugates of arginine-rich peptides with two ATP mimetic scaffolds were synthesized and tested as inhibitors of Pim-1. Against a panel of 124 protein kinases, a novel ARC-PIM conjugate selectively inhibited PKs of the Pim family.

Original publication

DOI

10.1002/cmdc.201300042

Type

Journal article

Journal

ChemMedChem

Publication Date

06/2013

Volume

8

Pages

909 - 913

Keywords

Dose-Response Relationship, Drug, Molecular Structure, Nanostructures, Protein Kinase Inhibitors, Proto-Oncogene Proteins c-pim-1, Structure-Activity Relationship