… the art human protein kinase allosteric inhibitors that directly or indirectly target the αC helix
and we … of kinase–modulator complexes targeting the allosteric binding sites proximal to the …

… of numerous protein kinases is allosterically modulated by … αC helices), the αC helix plays
a key role in switching protein … In all examples, the displacement of the αC helix stabilizes …

… protein kinase regulation limited to their kinase domain only. From the functional point of view,
protein kinases … (C) The C terminus of the αC-helix in all kinases is anchored to the kinase …

… and αC helix in/out in the active/inactive protein kinase. Different orientations of DFG motif
and αC helix in … Besides, the displaced αC helix and Arg 255 together trap the most N-terminal …

… helix αC is formed. Due to requirements of the catalytic mechanism, the active kinase
conformation is very similar among protein kinases… -competitive kinase inhibitors by replacement …

… Due to their critical role in cellular signaling, protein kinases … allosteric back pocket ligands
require a displaced αC-helix … the discovery of allosteric modulators for two kinases, and the dif…

… a protein kinase, this DFG-motif occupies a hydrophobic back pocket adjacent to the ATP
binding site next to the αC-helix of … Some general approaches for activation and inhibition have …

… and discovery of kinase inhibitors and allosteric modulators of kinase activation. The lessons
… -in/αChelix-out kinase conformation, in which the αC-helix is displaced outwards from the …

… the druggability of an allosteric site called the helix αC patch. … binding assay that monitors
the displacement of a fluorophore-… the PIF pocket, so allosteric modulation of PDK1 activity by …

… helix incorporates portions of both CBDs, including the αB and αC helices from CBD-A and
the αN helix … indication of this flexibility, because the displacement of CBD-B relative to CBD-A…