TY - DATA T1 - An Aptamer to the MAP Kinase Insert Region PY - 2015/01/16 AU - Sabine Lennarz AU - Elena Heider AU - Michael Blind AU - Günter Mayer UR - https://acs.figshare.com/articles/journal_contribution/An_Aptamer_to_the_MAP_Kinase_Insert_Region/2214982 DO - 10.1021/cb5005756.s001 L4 - https://ndownloader.figshare.com/files/3850558 KW - block domain KW - protein kinase inhibitors KW - protein kinases KW - RNA aptamers KW - drug discovery KW - function KW - kinase inhibitors KW - chemical biology research KW - weight compounds KW - MAP Kinase Insert RegionTargeting KW - kinase activity N2 - 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. ER -