List of works - John Tesmer

A GAIN in understanding autoproteolytic G protein-coupled receptors and polycystic kidney disease proteins ⬇️

scientific article published on March 2, 2012

A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor

scientific article published on 31 March 2020

A Receptor on Acid.

scientific article published in January 2017

A conserved hydrophobic surface of the LARG pleckstrin homology domain is critical for RhoA activation in cells.

scientific article published on 26 June 2009

A new approach to producing functional G alpha subunits yields the activated and deactivated structures of G alpha(12/13) proteins

scientific article

A retractable lid in lecithin:cholesterol acyltransferase provides a structural mechanism for activation by apolipoprotein A-I.

scientific article published on 13 October 2017

Activation of G Protein-Coupled Receptor Kinase 1 Involves Interactions between Its N-Terminal Region and Its Kinase Domain ⬇️

scientific article published on February 22, 2011

C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor

scientific article published on 24 April 2015

Characterization of GRK2 RH domain-dependent regulation of GPCR coupling to heterotrimeric G proteins

scientific article published on 01 January 2004

Cluster cytometry for high-capacity bioanalysis.

scientific article published on 21 March 2012

Conserved modular domains team up to latch-open active protein kinase Cα

scientific article

Constitutively active rhodopsin mutants causing night blindness are effectively phosphorylated by GRKs but differ in arrestin-1 binding

scientific article published on 17 July 2013

Correction to "Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine"

scientific article published on 12 June 2019

Cryo-electron microscopy structure and analysis of the P-Rex1-Gβγ signaling scaffold

scientific article published on 16 October 2019

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor

scientific article

Crystal structure of the adenylyl cyclase activator Gsalpha

scientific article published in December 1997

Crystal structure of the catalytic domains of adenylyl cyclase in a complex with Gsalpha.GTPgammaS

scientific article published in December 1997

Crystallization of Complex between Soluble Domains of Adenylyl Cyclase and Activated Gsα ⬇️

scientific article published on January 1, 2002

Crystallographic Pursuit of a Protein-RNA Aptamer Complex

scientific article

Determinants of pH profile and acyl chain selectivity in lysosomal phospholipase A2.

scientific article

Discovery of Small Molecules That Target the Phosphatidylinositol (3,4,5) Trisphosphate (PIP3)-Dependent Rac Exchanger 1 (P-Rex1) PIP3-Binding Site and Inhibit P-Rex1-Dependent Functions in Neutrophils

scientific article published on 03 January 2020

Effect of Lipid Composition on the Membrane Orientation of the G Protein-Coupled Receptor Kinase 2-Gβ1γ2 Complex

scientific article published on 18 April 2016

Exchange of Substrate and Inhibitor Specificities between Adenylyl and Guanylyl Cyclases ⬇️

scientific article published on June 26, 1998

Feedback inhibition of G protein-coupled receptor kinase 2 (GRK2) activity by extracellular signal-regulated kinases.

scientific article

G Protein-Coupled Receptor Kinase 2 (GRK2) and 5 (GRK5) Exhibit Selective Phosphorylation of the Neurotensin Receptor in Vitro

scientific article published on 8 July 2015

G protein-coupled receptor Kinase 2/G alpha q/11 interaction. A novel surface on a regulator of G protein signaling homology domain for binding G alpha subunits.

scientific article published on 8 November 2002

GRK2 activation by receptors: role of the kinase large lobe and carboxyl-terminal tail.

scientific article published on May 2009

Galpha q allosterically activates and relieves autoinhibition of p63RhoGEF.

scientific article

Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors

scientific article published on 04 January 2021

Guanylyl cyclase sees the light.

scientific article

Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes.

scientific article published on 20 April 2016

Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor

scientific article

Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors

scientific article

Identification of a Gialpha binding site on type V adenylyl cyclase

scientific article

In Situ Investigation of Heterotrimeric G Protein βγ Subunit Binding and Orientation on Membrane Bilayers

article

Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma

scientific article (publication date: 23 May 2003)

Lecithin:Cholesterol Acyltransferase Activation by Sulfhydryl-Reactive Small Molecules: Role of Cysteine-31.

scientific article published on 02 June 2017

Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays

scientific article

Membrane orientation and binding determinants of G protein-coupled receptor kinase 5 as assessed by combined vibrational spectroscopic studies.

scientific article

Molecular basis for P-site inhibition of adenylyl cyclase

scientific article

Molecular basis for activation of G protein-coupled receptor kinases ⬇️

scientific article published on August 20, 2010

Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol

scientific article published on 27 November 2018

Molecular basis for small molecule inhibition of G protein-coupled receptor kinases

scientific article

Molecular mechanisms of phospholipase C β3 autoinhibition.

scientific article

Monomeric rhodopsin is sufficient for normal rhodopsin kinase (GRK1) phosphorylation and arrestin-1 binding

scientific article

Navigating the conformational landscape of G protein-coupled receptor kinases during allosteric activation.

scientific article

Paroxetine Is a Direct Inhibitor of G Protein-Coupled Receptor Kinase 2 and Increases Myocardial Contractility ⬇️

scientific article published on August 21, 2012

Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe

scientific article published on 23 July 2019

Phospholipid Component Defines Pharmacokinetic and Pharmacodynamic Properties of Synthetic High-Density Lipoproteins

scientific article published on 27 November 2019

Plasma membrane association of p63 Rho guanine nucleotide exchange factor (p63RhoGEF) is mediated by palmitoylation and is required for basal activity in cells

scientific article

Preferential hydrolysis of truncated oxidized glycerophospholipids by lysosomal phospholipase A2.

scientific article published on 19 December 2016

Preliminary X-ray analysis of Escherichia coli GMP synthetase: determination of anomalous scattering factors for a cysteinyl mercury derivative.

scientific article

Preliminary structure analysis of the DH/PH domains of leukemia-associated RhoGEF.

scientific article

Protein-ligand energetics assessed using deoxy and fluorodeoxy sugars in equilibrium binding and high resolution crystallographic studies

scientific article published on 01 August 1992

Quantitative Multiple-Reaction Monitoring Proteomic Analysis of Gβ and Gγ Subunits in C57Bl6/J Brain Synaptosomes.

scientific article

Recognition in the face of diversity: interactions of heterotrimeric G proteins and G protein-coupled receptor (GPCR) kinases with activated GPCRs

scientific article

Regulation of G Protein-Coupled Receptor Kinases by Phospholipids

scientific article published on January 1, 2013

Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.

scientific article

Structural analysis of lecithin:cholesterol acyltransferase bound to high density lipoprotein particles

scientific article published on 15 January 2020

Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3.

scientific article published on 11 April 2016

Structural and Functional Analysis of G Protein-Coupled Receptor Kinase Inhibition by Paroxetine and a Rationally Designed Analog

scientific article

Structural insights into G protein-coupled receptor kinase function.

scientific article

Structural insights into phospholipase C-β function.

scientific article published on 23 July 2013

Structure and function of lysosomal phospholipase A2 and lecithin:cholesterol acyltransferase.

scientific article

Structure of RGS4 bound to AlF4--activated G(i alpha1): stabilization of the transition state for GTP hydrolysis

scientific article

Structure of the C-terminal guanine nucleotide exchange factor module of Trio in an autoinhibited conformation reveals its oncogenic potential

scientific article published on 19 February 2019

Structure of the Regulator of G Protein Signaling 8 (RGS8)-Gαq Complex: MOLECULAR BASIS FOR Gα SELECTIVITY.

scientific article

Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.

scientific article

Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.

scientific article

Substrate-Induced Changes in the Dynamics of Rhodopsin Kinase (G Protein-Coupled Receptor Kinase 1) ⬇️

scientific article published on April 11, 2012

Subunit Stabilization and Polyethylene Glycolation of Cocaine Esterase Improves In Vivo Residence Time ⬇️

scientific article published on September 2, 2011

The crystal structure of GMP synthetase reveals a novel catalytic triad and is a structural paradigm for two enzyme families

scientific article

The first DEP domain of the RhoGEF P-Rex1 autoinhibits activity andcontributes to membrane binding

scientific article published on 13 July 2020

The role of G beta gamma and domain interfaces in the activation of G protein-coupled receptor kinase 2.

scientific article published in May 2005

The structure, catalytic mechanism and regulation of adenylyl cyclase

scientific article published on 01 December 1998

Tracking the Cartoon mouse phenotype: Hemopexin domain-dependent regulation of MT1-MMP pericellular collagenolytic activity

scientific article published on 11 April 2018

Trio's Rho-specific GEF domain is the missing Galpha q effector in C. elegans

scientific article

Unique hydrophobic extension of the RGS2 amphipathic helix domain imparts increased plasma membrane binding and function relative to other RGS R4/B subfamily members.

scientific article published on 11 September 2007

Unveiling the membrane-binding properties of N-terminal and C-terminal regions of G protein-coupled receptor kinase 5 by combined optical spectroscopies

scientific article published on 16 January 2014

Using iterative fragment assembly and progressive sequence truncation to facilitate phasing and crystal structure determination of distantly related proteins

scientific article

Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.

scientific article published on 30 March 2018

List of works by John Tesmer

A GAIN in understanding autoproteolytic G protein-coupled receptors and polycystic kidney disease proteins ⬇️

A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor

A Receptor on Acid.

A conserved hydrophobic surface of the LARG pleckstrin homology domain is critical for RhoA activation in cells.

A new approach to producing functional G alpha subunits yields the activated and deactivated structures of G alpha(12/13) proteins

A retractable lid in lecithin:cholesterol acyltransferase provides a structural mechanism for activation by apolipoprotein A-I.

Activation of G Protein-Coupled Receptor Kinase 1 Involves Interactions between Its N-Terminal Region and Its Kinase Domain ⬇️

C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor

Characterization of GRK2 RH domain-dependent regulation of GPCR coupling to heterotrimeric G proteins

Cluster cytometry for high-capacity bioanalysis.

Conserved modular domains team up to latch-open active protein kinase Cα

Constitutively active rhodopsin mutants causing night blindness are effectively phosphorylated by GRKs but differ in arrestin-1 binding

Correction to "Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine"

Cryo-electron microscopy structure and analysis of the P-Rex1-Gβγ signaling scaffold

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor

Crystal structure of the adenylyl cyclase activator Gsalpha

Crystal structure of the catalytic domains of adenylyl cyclase in a complex with Gsalpha.GTPgammaS

Crystallization of Complex between Soluble Domains of Adenylyl Cyclase and Activated Gsα ⬇️

Crystallographic Pursuit of a Protein-RNA Aptamer Complex

Determinants of pH profile and acyl chain selectivity in lysosomal phospholipase A2.

Discovery of Small Molecules That Target the Phosphatidylinositol (3,4,5) Trisphosphate (PIP3)-Dependent Rac Exchanger 1 (P-Rex1) PIP3-Binding Site and Inhibit P-Rex1-Dependent Functions in Neutrophils

Effect of Lipid Composition on the Membrane Orientation of the G Protein-Coupled Receptor Kinase 2-Gβ1γ2 Complex

Exchange of Substrate and Inhibitor Specificities between Adenylyl and Guanylyl Cyclases ⬇️

Feedback inhibition of G protein-coupled receptor kinase 2 (GRK2) activity by extracellular signal-regulated kinases.

G Protein-Coupled Receptor Kinase 2 (GRK2) and 5 (GRK5) Exhibit Selective Phosphorylation of the Neurotensin Receptor in Vitro

G protein-coupled receptor Kinase 2/G alpha q/11 interaction. A novel surface on a regulator of G protein signaling homology domain for binding G alpha subunits.

GRK2 activation by receptors: role of the kinase large lobe and carboxyl-terminal tail.

Galpha q allosterically activates and relieves autoinhibition of p63RhoGEF.

Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors

Guanylyl cyclase sees the light.

Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes.

Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor

Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors

Identification of a Gialpha binding site on type V adenylyl cyclase

In Situ Investigation of Heterotrimeric G Protein βγ Subunit Binding and Orientation on Membrane Bilayers

Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma

Lecithin:Cholesterol Acyltransferase Activation by Sulfhydryl-Reactive Small Molecules: Role of Cysteine-31.

Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays

Membrane orientation and binding determinants of G protein-coupled receptor kinase 5 as assessed by combined vibrational spectroscopic studies.

Molecular basis for P-site inhibition of adenylyl cyclase

Molecular basis for activation of G protein-coupled receptor kinases ⬇️

Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol

Molecular basis for small molecule inhibition of G protein-coupled receptor kinases

Molecular mechanisms of phospholipase C β3 autoinhibition.

Monomeric rhodopsin is sufficient for normal rhodopsin kinase (GRK1) phosphorylation and arrestin-1 binding

Navigating the conformational landscape of G protein-coupled receptor kinases during allosteric activation.

Paroxetine Is a Direct Inhibitor of G Protein-Coupled Receptor Kinase 2 and Increases Myocardial Contractility ⬇️

Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe

Phospholipid Component Defines Pharmacokinetic and Pharmacodynamic Properties of Synthetic High-Density Lipoproteins

Plasma membrane association of p63 Rho guanine nucleotide exchange factor (p63RhoGEF) is mediated by palmitoylation and is required for basal activity in cells

Preferential hydrolysis of truncated oxidized glycerophospholipids by lysosomal phospholipase A2.

Preliminary X-ray analysis of Escherichia coli GMP synthetase: determination of anomalous scattering factors for a cysteinyl mercury derivative.

Preliminary structure analysis of the DH/PH domains of leukemia-associated RhoGEF.

Protein-ligand energetics assessed using deoxy and fluorodeoxy sugars in equilibrium binding and high resolution crystallographic studies

Quantitative Multiple-Reaction Monitoring Proteomic Analysis of Gβ and Gγ Subunits in C57Bl6/J Brain Synaptosomes.

Recognition in the face of diversity: interactions of heterotrimeric G proteins and G protein-coupled receptor (GPCR) kinases with activated GPCRs

Regulation of G Protein-Coupled Receptor Kinases by Phospholipids

Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.

Structural analysis of lecithin:cholesterol acyltransferase bound to high density lipoprotein particles

Structural and Biochemical Characterization of the Catalytic Core of the Metastatic Factor P-Rex1 and Its Regulation by PtdIns(3,4,5)P3.

Structural and Functional Analysis of G Protein-Coupled Receptor Kinase Inhibition by Paroxetine and a Rationally Designed Analog

Structural insights into G protein-coupled receptor kinase function.

Structural insights into phospholipase C-β function.

Structure and function of lysosomal phospholipase A2 and lecithin:cholesterol acyltransferase.

Structure of RGS4 bound to AlF4--activated G(i alpha1): stabilization of the transition state for GTP hydrolysis

Structure of the C-terminal guanine nucleotide exchange factor module of Trio in an autoinhibited conformation reveals its oncogenic potential

Structure of the Regulator of G Protein Signaling 8 (RGS8)-Gαq Complex: MOLECULAR BASIS FOR Gα SELECTIVITY.

Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.

Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.

Substrate-Induced Changes in the Dynamics of Rhodopsin Kinase (G Protein-Coupled Receptor Kinase 1) ⬇️

Subunit Stabilization and Polyethylene Glycolation of Cocaine Esterase Improves In Vivo Residence Time ⬇️

The crystal structure of GMP synthetase reveals a novel catalytic triad and is a structural paradigm for two enzyme families

The first DEP domain of the RhoGEF P-Rex1 autoinhibits activity andcontributes to membrane binding

The role of G beta gamma and domain interfaces in the activation of G protein-coupled receptor kinase 2.

The structure, catalytic mechanism and regulation of adenylyl cyclase

Tracking the Cartoon mouse phenotype: Hemopexin domain-dependent regulation of MT1-MMP pericellular collagenolytic activity

Trio's Rho-specific GEF domain is the missing Galpha q effector in C. elegans

Unique hydrophobic extension of the RGS2 amphipathic helix domain imparts increased plasma membrane binding and function relative to other RGS R4/B subfamily members.

Unveiling the membrane-binding properties of N-terminal and C-terminal regions of G protein-coupled receptor kinase 5 by combined optical spectroscopies