A moving target: structure and disorder in pursuit of Myc inhibitors

R Bayliss, SG Burgess, E Leen… - Biochemical Society …, 2017 - portlandpress.com
The Myc proteins comprise a family of ubiquitous regulators of gene expression implicated
in over half of all human cancers. They interact with a large number of other proteins, such …

Exploring the conformational landscapes of protein kinases: perspectives from FRET and DEER

ZD Baker, DM Rasmussen… - Biochemical Society …, 2024 - portlandpress.com
Conformational changes of catalytically-important structural elements are a key feature of
the regulation mechanisms of protein kinases and are important for dictating inhibitor …

Dynamic equilibria in protein kinases

LM Pegram, JW Anderson, NG Ahn - Current opinion in structural biology, 2021 - Elsevier
Structural changes involved in protein kinase activation and ligand binding have been
determined from a wealth of X-ray crystallographic evidence. Recent solution studies using …

Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α

P Roser, J Weisner, JR Simard, D Rauh… - Chemical …, 2018 - pubs.rsc.org
Conformational transitions in protein kinases are crucial for the biological function of these
enzymes. Here, we characterize and assess conformational equilibria of the activation loop …

Tracking protein domain movements by EPR distance determination and multilateration

J Stehle, M Drescher - Methods in Enzymology, 2022 - Elsevier
Electron paramagnetic resonance (EPR) spectroscopy in combination with site-directed spin
labeling (SDSL) is a powerful approach to supplement the large toolbox of methods for …