cb5005756_si_001.pdf (1.95 MB)
An Aptamer to the MAP Kinase Insert Region
journal contribution
posted on 2015-01-16, 00:00 authored by Sabine Lennarz, Elena Heider, Michael Blind, Günter MayerTargeting
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.