Kinase activation by small conformational changes

ED Lopez, O Burastero, JP Arcon… - Journal of chemical …, 2019 - ACS Publications
Protein kinases (PKs) are allosteric enzymes that play an essential role in signal
transduction by regulating a variety of key cellular processes. Most PKs suffer …

Activation loop plasticity and active site coupling in the MAP kinase, ERK2

L Pegram, D Riccardi, N Ahn - Journal of Molecular Biology, 2023 - Elsevier
Previous studies of the protein kinase, ERK2, using NMR and hydrogen-exchange
measurements have shown changes in dynamics accompanying its activation by …

Activation loop dynamics are controlled by conformation-selective inhibitors of ERK2

LM Pegram, JC Liddle, Y Xiao, M Hoh… - Proceedings of the …, 2019 - National Acad Sciences
Conformational selection by small molecules expands inhibitory possibilities for protein
kinases. Nuclear magnetic resonance (NMR) measurements of the mitogen-activated …

Solution NMR insights into docking interactions involving inactive ERK2

A Piserchio, M Warthaka, AK Devkota, TS Kaoud… - Biochemistry, 2011 - ACS Publications
The mitogen-activated protein (MAP) kinase ERK2 contains recruitment sites that engage
canonical and noncanonical motifs found in a variety of upstream kinases, regulating …

[HTML][HTML] Probing conformational dynamics to understand kinase inhibition

IR Outhwaite, MA Seeliger - Elife, 2023 - elifesciences.org
Kinase Activity: Probing conformational dynamics to understand kinase inhibition | eLife Skip to
Content eLife logo eLife home page Menu Home Magazine Community About Search Alerts …

[HTML][HTML] Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2

JW Anderson, D Vaisar, DN Jones, LM Pegram… - Elife, 2024 - elifesciences.org
Activation of the extracellular signal-regulated kinase-2 (ERK2) by phosphorylation has
been shown to involve changes in protein dynamics, as determined by hydrogen-deuterium …

Extracellular-regulated kinase 2 is activated by the enhancement of hinge flexibility

KM Sours, Y Xiao, NG Ahn - Journal of molecular biology, 2014 - Elsevier
Protein motions underlie conformational and entropic contributions to enzyme catalysis;
however, relatively little is known about the ways in which this occurs. Studies of the mitogen …

Activation loop dynamics are coupled to core motions in extracellular signal-regulated kinase-2

DB Iverson, Y Xiao, DN Jones, EZ Eisenmesser… - Biochemistry, 2020 - ACS Publications
The activation loop segment in protein kinases is a common site for regulatory
phosphorylation. In extracellular signal-regulated kinase 2 (ERK2), dual phosphorylation …

[HTML][HTML] The autoinhibited state of MKK4: Phosphorylation, putative dimerization and R134W mutant studied by molecular dynamics simulations

E Shevchenko, A Poso, T Pantsar - Computational and Structural …, 2020 - Elsevier
Protein kinases are crucial components of the cell-signalling machinery that orchestrate and
convey messages to their downstream targets. Most often, kinases are activated upon a …

How mitogen-activated protein kinases recognize and phosphorylate their targets: A QM/MM study

AG Turjanski, G Hummer… - Journal of the American …, 2009 - ACS Publications
Mitogen-activated protein kinase (MAPK) signaling pathways play an essential role in the
transduction of environmental stimuli to the nucleus, thereby regulating a variety of cellular …