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

Journal Article · · Proc. Natl. Acad. Sci. USA

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; National Institutes of Health (NIH)
OSTI ID:
1836728
Journal Information:
Proc. Natl. Acad. Sci. USA, Vol. 116, Issue (31)
Country of Publication:
United States
Language:
ENGLISH

References (36)

Circumventing Cancer Drug Resistance in the Era of Personalized Medicine journal February 2012
Development of Extracellular Signal-Regulated Kinase Inhibitors journal May 2009
Targeting RAS -mutant Cancers: Is ERK the Key? journal November 2015
Atomic structure of the MAP kinase ERK2 at 2.3 Å resolution journal February 1994
Activation Mechanism of the MAP Kinase ERK2 by Dual Phosphorylation journal September 1997
Docking Motif Interactions in MAP Kinases Revealed by Hydrogen Exchange Mass Spectrometry journal April 2004
The Conformational Plasticity of Protein Kinases journal May 2002
Defining a new nomenclature for the structures of active and inactive kinases journal March 2019
Changes in protein conformational mobility upon activation of extracellular regulated protein kinase-2 as detected by hydrogen exchange journal January 2001
Dynamics of Protein Kinases: Insights from Nuclear Magnetic Resonance journal March 2015
Phosphorylation releases constraints to domain motion in ERK2 journal February 2014
Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control journal September 2009
Slow Inhibition and Conformation Selective Properties of Extracellular Signal-Regulated Kinase 1 and 2 Inhibitors journal December 2014
Hydrogen Exchange Solvent Protection by an ATP Analogue Reveals Conformational Changes in ERK2 upon Activation journal October 2005
Extracellular-Regulated Kinase 2 Is Activated by the Enhancement of Hinge Flexibility journal May 2014
Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery? journal April 2014
Discovery of ( S )-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1 H -pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1 H )-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development journal June 2016
Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors journal April 2013
Metal coordination in kinases and pseudokinases journal June 2017
Structure of extracellular signal-regulated kinase 2 in complex with ATP and ADP journal November 2012
Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors journal June 2017
Intrinsically active variants of Erk oncogenically transform cells and disclose unexpected autophosphorylation capability that is independent of TEY phosphorylation journal March 2016
Importance of Domain Closure for the Autoactivation of ERK2 journal August 2011
A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics journal September 2014
Protein hydrogen exchange mechanism: Local fluctuations journal January 2003
Specificity of Phosphorylation Responses to Mitogen Activated Protein (MAP) Kinase Pathway Inhibitors in Melanoma Cells journal December 2017
The Mechanism of Dephosphorylation of Extracellular Signal-regulated Kinase 2 by Mitogen-activated Protein Kinase Phosphatase 3 journal August 2001
Physiological Concentrations of Divalent Magnesium Ion Activate the Serine/Threonine Specific Protein Kinase ERK2 journal February 2003
Contribution of Surface Salt Bridges to Protein Stability , journal January 2000
Direct monitoring of the conformational equilibria of the activation loop in the mitogen-activated protein kinase p38α journal January 2018
Towards simple kinetic models of functional dynamics for a kinase subfamily journal July 2018
Dynamic Equilibrium of the Aurora A Kinase Activation Loop Revealed by Single-Molecule Spectroscopy journal August 2017
A dynamic mechanism for allosteric activation of Aurora kinase A by activation loop phosphorylation journal February 2018
Ligand discrimination between active and inactive activation loop conformations of Aurora-A kinase is unmodified by phosphorylation journal January 2019
Quantitative conformational profiling of kinase inhibitors reveals origins of selectivity for Aurora kinase activation states journal December 2018
Conformation-Selective ATP-Competitive Inhibitors Control Regulatory Interactions and Noncatalytic Functions of Mitogen-Activated Protein Kinases journal May 2014