Journal
ACS CHEMICAL BIOLOGY
Volume 10, Issue 1, Pages 320-327Publisher
AMER CHEMICAL SOC
DOI: 10.1021/cb5005756
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Funding
- NRW LIMES Graduate School Chemical Biology
- European Research Council under the European Union/ERC [615381]
- European Research Council (ERC) [615381] Funding Source: European Research Council (ERC)
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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 proteinprotein 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.
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