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How ATP-Competitive Inhibitors Allosterically Modulate Tyrosine Kinases That Contain a Src-like Regulatory Architecture

Journal Article · · ACS Chemical Biology

Research Organization:
Brookhaven National Lab. (BNL), Upton, NY (United States)
Sponsoring Organization:
~OTHER
DOE Contract Number:
SC0012704
OSTI ID:
1690205
Report Number(s):
BNL-220526-2020-JACI
Journal Information:
ACS Chemical Biology, Vol. 15, Issue 7
Country of Publication:
United States
Language:
English

References (50)

Evolution of the eukaryotic protein kinases as dynamic molecular switches journal September 2012
The Protein Kinase Complement of the Human Genome journal December 2002
The origin of protein interactions and allostery in colocalization journal December 2007
Protein–protein interactions in the allosteric regulation of protein kinases journal December 2006
Structural Basis for the Non-catalytic Functions of Protein Kinases journal January 2016
The Conformational Plasticity of Protein Kinases journal May 2002
Protein kinases: evolution of dynamic regulatory proteins journal February 2011
Structure and dynamic regulation of Src-family kinases journal June 2008
Structures of Src-family tyrosine kinases journal December 1997
Src kinases as therapeutic targets for cancer journal October 2009
Catalytic Control in the EGF Receptor and Its Connection to General Kinase Regulatory Mechanisms journal April 2011
Structure and regulation of Src family kinases journal October 2004
Chemoproteomic Method for Profiling Inhibitor-Bound Kinase Complexes journal June 2019
A Combined Approach Reveals a Regulatory Mechanism Coupling Src’s Kinase Activity, Localization, and Phosphotransferase-Independent Functions journal April 2019
Dynamic Coupling between the SH2 and SH3 Domains of c-Src and Hck Underlies Their Inactivation by C-Terminal Tyrosine Phosphorylation journal April 2001
Crystal Structures of c-Src Reveal Features of Its Autoinhibitory Mechanism journal May 1999
Targeting Dynamic ATP-Binding Site Features Allows Discrimination between Highly Homologous Protein Kinases journal April 2019
Divergent Modulation of Src-Family Kinase Regulatory Interactions with ATP-Competitive Inhibitors journal July 2014
Active site profiling reveals coupling between domains in SRC-family kinases journal November 2012
SH2-Catalytic Domain Linker Heterogeneity Influences Allosteric Coupling across the SFK Family journal October 2014
Survey of solution dynamics in Src kinase reveals allosteric cross talk between the ligand binding and regulatory sites journal December 2017
Selective Proteolysis to Study the Global Conformation and Regulatory Mechanisms of c-Src Kinase journal June 2019
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity journal March 2016
c-Src Binds to the Cancer Drug Imatinib with an Inactive Abl/c-Kit Conformation and a Distributed Thermodynamic Penalty journal March 2007
NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors journal November 2013
A Myristoyl/Phosphotyrosine Switch Regulates c-Abl journal March 2003
Structural Basis for the Autoinhibition of c-Abl Tyrosine Kinase journal March 2003
Organization of the SH3-SH2 Unit in Active and Inactive Forms of the c-Abl Tyrosine Kinase journal March 2006
ATP Site Ligands Determine the Assembly State of the Abelson Kinase Regulatory Core via the Activation Loop Conformation journal January 2018
Targeting Conformational Plasticity of Protein Kinases journal December 2014
Small Molecule Recognition of c-Src via the Imatinib-Binding Conformation journal October 2008
Structural differences between repressed and derepressed forms of p60c-src. journal June 1989
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases journal October 2008
Chemical genetic strategy for targeting protein kinases based on covalent complementarity journal August 2011
Structure-Guided Inhibitor Design Expands the Scope of Analog-Sensitive Kinase Technology journal July 2013
A conserved protonation-dependent switch controls drug binding in the Abl kinase journal December 2008
Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations journal March 2009
A Chemical-Genetic Approach to Generate Selective Covalent Inhibitors of Protein Kinases journal April 2017
A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases journal May 2005
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors journal August 2007
Kinobead and Single-Shot LC-MS Profiling Identifies Selective PKD Inhibitors journal February 2017
Kinome chemoproteomics characterization of pyrrolo[3,4- c ]pyrazoles as potent and selective inhibitors of glycogen synthase kinase 3 journal January 2018
A short history of blebbing journal September 2008
Structural mechanism for Bruton’s tyrosine kinase activation at the cell membrane journal April 2019
Autoinhibition of Bruton's tyrosine kinase (Btk) and activation by soluble inositol hexakisphosphate journal February 2015
N-Myristoylated c-Abl Tyrosine Kinase Localizes to the Endoplasmic Reticulum upon Binding to an Allosteric Inhibitor journal October 2009
Structure, Regulation, Signaling, and Targeting of Abl Kinases in Cancer journal May 2012
Phosphatidylinositol 3-Kinase-dependent Membrane Association of the Bruton's Tyrosine Kinase Pleckstrin Homology Domain Visualized in Single Living Cells journal April 1999
Targeting ABL-IRE1α Signaling Spares ER-Stressed Pancreatic β Cells to Reverse Autoimmune Diabetes journal April 2017
BTK Regulates PtdIns-4,5-P2 Synthesis journal November 2003