Abstract
The conformational dynamics of a kinase's activation loop have been challenging to assess due to the activation loop's intrinsic flexibility. To directly probe the conformational equilibrium of the activation loop of mitogen-activated protein kinase p38α, we present an approach based on site-directed spin labeling, electron paramagnetic resonance (EPR) distance restraints, and multilateration. We demonstrate that the activation loop of apo p38α resides in a highly flexible equilibrium state and we reveal that binding of small molecules significantly alters this equilibrium and the populated sub-states.
Highlights
Patrick Roser, ‡a Jorn Weisner, ‡b Juliane Stehle, a Daniel Rauh *b and Malte Drescher *a
To directly probe the conformational equilibrium of the activation loop of mitogen-activated protein kinase p38a, we present an approach based on site-directed spin labeling, electron paramagnetic resonance (EPR) distance restraints, and multilateration
We demonstrate that the activation loop of apo p38a resides in a highly flexible equilibrium state and we reveal that binding of small molecules significantly alters this equilibrium and the populated sub-states
Summary
Patrick Roser, ‡a Jorn Weisner, ‡b Juliane Stehle, a Daniel Rauh *b and Malte Drescher *a. To directly probe the conformational equilibrium of the activation loop of mitogen-activated protein kinase p38a, we present an approach based on site-directed spin labeling, electron paramagnetic resonance (EPR) distance restraints, and multilateration.
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