Selective Bisubstrate Inhibitors with Sub‐nanomolar Affinity for Protein Kinase Pim‐1 | Zendy

Ekambaram Ramesh | Zendy; Enkvist Erki | Zendy; Vaasa Angela | Zendy; Kasari Marje | Zendy; Raidaru Gerda | Zendy; Knapp Stefan | Zendy; Uri Asko | Zendy

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Selective Bisubstrate Inhibitors with Sub‐nanomolar Affinity for Protein Kinase Pim‐1

Author(s) -

Ekambaram Ramesh,

Enkvist Erki,

Vaasa Angela,

Kasari Marje,

Raidaru Gerda,

Knapp Stefan,

Uri Asko

Publication year - 2013

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.201300042

Subject(s) - kinase , conjugate , chemistry , biochemistry , computational biology , combinatorial chemistry , biology , mathematical analysis , mathematics

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.

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