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ACS Chem Biol. 2015 Jan 16;10(1):320-7. doi: 10.1021/cb5005756. Epub 2014 Sep 11.

An aptamer to the MAP kinase insert region.

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Life and Medical Sciences Institute , Gerhard-Domagk-Str.1, 53121 Bonn, Germany.


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.

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