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Selective bisubstrate inhibitors with sub-nanomolar affinity for protein kinase Pim-1. 2013

Ramesh Ekambaram, and Erki Enkvist, and Angela Vaasa, and Marje Kasari, and Gerda Raidaru, and Stefan Knapp, and Asko Uri
Institute of Chemistry, University of Tartu, Tartu, Estonia.

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.

UI MeSH Term Description Entries
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D047428 Protein Kinase Inhibitors Agents that inhibit PROTEIN KINASES. Protein Kinase Inhibitor,Inhibitor, Protein Kinase,Inhibitors, Protein Kinase,Kinase Inhibitor, Protein,Kinase Inhibitors, Protein
D049329 Nanostructures Materials which have structured components with at least one dimension in the range of 1 to 100 nanometers. These include NANOCOMPOSITES; NANOPARTICLES; NANOTUBES; and NANOWIRES. Nanomaterials,Nanostructured Materials,Material, Nanostructured,Materials, Nanostructured,Nanomaterial,Nanostructure,Nanostructured Material
D051573 Proto-Oncogene Proteins c-pim-1 Serine-threonine protein kinases that relay signals from CYTOKINE RECEPTORS and are involved in control of CELL GROWTH PROCESSES; CELL DIFFERENTIATION; and APOPTOSIS. c-pim-1 Protein,pim-1 Proto-Oncogene Protein,Pim-1 Kinase,Proto-Oncogene Protein c-pim-1,Proto-Oncogene Protein pim-1,Kinase, Pim-1,Pim 1 Kinase,Proto Oncogene Protein c pim 1,Proto Oncogene Protein pim 1,Proto Oncogene Proteins c pim 1,c pim 1 Protein,c-pim-1, Proto-Oncogene Protein,c-pim-1, Proto-Oncogene Proteins,pim 1 Proto Oncogene Protein,pim-1, Proto-Oncogene Protein

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