An aptamer to the MAP kinase insert region
| Autor: | Sabine Lennarz, Michael Blind, Günter Mayer, Elena Heider |
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| Rok vydání: | 2014 |
| Předmět: |
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Molecular Aptamer Molecular Sequence Data Chemical biology Computational biology Biochemistry Insert (molecular biology) Drug Discovery Escherichia coli Humans Kinase activity Protein kinase A Protein Kinase Inhibitors Mitogen-Activated Protein Kinase 1 Binding Sites biology Base Sequence Kinase Drug discovery General Medicine Aptamers Nucleotide Recombinant Proteins 3. Good health Mitogen-activated protein kinase biology.protein Molecular Medicine Protein Binding |
| Zdroj: | ACS chemical biology. 10(1) |
| ISSN: | 1554-8937 |
| Popis: | Targeting functional, non-catalytic domains of protein kinases or other proteins is an emerging field in chemical biology research. Non-ATP competitive kinase inhibitors allow for the investigation of active-site independent functions, e.g., the biological role of protein–protein interactions. These inhibitors also serve as a starting point for developing novel therapeutic strategies. However, the identification of such inhibitors by means of conventional low molecular weight compounds represents a great challenge in modern drug discovery. Employing the mitogen-activated protein (MAP) kinase Erk2, we show that RNA aptamers have the capacity to be a novel, promising class of protein kinase inhibitors that can be applied to target individual subdomains and block domain specific functions without affecting kinase activity per se. |
| Databáze: | OpenAIRE |
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