Renaissance of allostery to disrupt protein kinase interactions
… 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 …
a key role in switching protein … In all examples, the displacement of the αC helix stabilizes …
Dual roles of ATP-binding site in protein kinases: Orthosteric inhibition and allosteric regulation
M Li, AU Rehman, Y Liu, K Chen, S Lu - … in Protein Chemistry and Structural …, 2021 - Elsevier
… 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 …
and αC helix in … Besides, the displaced αC helix and Arg 255 together trap the most N-terminal …
Expanding the opportunities for modulating kinase targets with allosteric approaches
H Mobitz, W Jahnke… - Current topics in …, 2017 - ingentaconnect.com
… 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…
require a displaced αC-helix … the discovery of allosteric modulators for two kinases, and the dif…
Leveraging structural diversity and allosteric regulatory mechanisms of protein kinases in the discovery of small molecule inhibitors
GM Verkhivker - Current Medicinal Chemistry, 2017 - ingentaconnect.com
… 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 …
… -in/αChelix-out kinase conformation, in which the αC-helix is displaced outwards from the …
Electrostatic interactions as mediators in the allosteric activation of protein kinase A RIα
E P. Barros, RD Malmstrom, K Nourbakhsh… - Biochemistry, 2017 - ACS Publications
… 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…
the αN helix … indication of this flexibility, because the displacement of CBD-B relative to CBD-A…
Allosteric modulation as a unifying mechanism for receptor function and regulation
JP Changeux, A Christopoulos - Diabetes, obesity and …, 2017 - Wiley Online Library
… protein-coupled receptors, nuclear hormone receptors and receptor tyrosine kinases are all
allosteric proteins … orientation of the “activation loop” and αC helix in the N-lobe of the TK to …
allosteric proteins … orientation of the “activation loop” and αC helix in the N-lobe of the TK to …
Interrogating regulatory mechanisms in signaling proteins by allosteric inhibitors and activators: a dynamic view through the lens of residue interaction networks
L Astl, A Tse, GM Verkhivker - Protein allostery in drug discovery, 2019 - Springer
… allosteric regulatory machinery of protein kinases and provide … , ordering or displacement of
the αC-helix, and modulation of … Although binding of allosteric modulators of protein kinases …
the αC-helix, and modulation of … Although binding of allosteric modulators of protein kinases …
Principles of kinase allosteric inhibition and pocket validation
Y Pan, MM Mader - Journal of medicinal chemistry, 2022 - ACS Publications
… by the α-C-helix displacement and the DFG motif characterized … Other more general
approaches to identify allosteric pockets … an alias for protein kinase AMP-activated catalytic …
approaches to identify allosteric pockets … an alias for protein kinase AMP-activated catalytic …
[HTML][HTML] Receptor Tyrosine Kinase KIT: Mutation-Induced Conformational Shift Promotes Alternative Allosteric Pockets
J Ledoux, M Botnari, L Tchertanov - Kinases and Phosphatases, 2023 - mdpi.com
… the Mitogen-Activated Protein Kinase (MAPK) signalling … decreased folding (3 10 -helix ↔
turn) and displaced β-hairpin. The … allosteric modulators bound to its area close to the αC-helix …
turn) and displaced β-hairpin. The … allosteric modulators bound to its area close to the αC-helix …
Allosteric regulation of protein kinases downstream of PI3-kinase signalling
AE Leroux, LZF Gross, M Sacerdoti… - Protein Allostery in Drug …, 2019 - Springer
… of protein kinases, which often involve the allosteric modulation … mediated by the helix αC
in many other protein kinases. … displaced the interaction of PDK1 with PIFtide allosterically but …
in many other protein kinases. … displaced the interaction of PDK1 with PIFtide allosterically but …