Format

Send to

Choose Destination
ChemMedChem. 2013 Jun;8(6):909-13. doi: 10.1002/cmdc.201300042. Epub 2013 Apr 24.

Selective bisubstrate inhibitors with sub-nanomolar affinity for protein kinase Pim-1.

Author information

1
Institute of Chemistry, University of Tartu, Tartu, Estonia.

Abstract

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.

PMID:
23616352
DOI:
10.1002/cmdc.201300042
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Wiley
Loading ...
Support Center