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

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.
Publication status:
Published

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Publisher copy:
10.1002/cmdc.201300042

Authors


Ekambaram, R More by this author
Enkvist, E More by this author
Raidaru, G More by this author
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Journal:
ChemMedChem
Volume:
8
Issue:
6
Pages:
909-913
Publication date:
2013-06-05
DOI:
EISSN:
1860-7187
ISSN:
1860-7179
URN:
uuid:a463db6f-e811-410e-b9dc-8ffbfe608182
Source identifiers:
405856
Local pid:
pubs:405856

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