Search Results - "Tesmer, John JG"
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Structural and dynamic changes in P-Rex1 upon activation by PIP3 and inhibition by IP4
Published in eLife (31-07-2024)“…PIP 3 -dependent Rac exchanger 1 (P-Rex1) is abundantly expressed in neutrophils and plays central roles in chemotaxis and cancer metastasis by serving as a…”
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2
Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol
Published in eLife (27-11-2018)“…Lecithin:cholesterol acyltransferase (LCAT) and LCAT-activating compounds are being investigated as treatments for coronary heart disease (CHD) and familial…”
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3
C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor
Published in eLife (24-04-2015)“…Rod photoreceptors generate measurable responses to single-photon activation of individual molecules of the G protein-coupled receptor (GPCR), rhodopsin…”
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4
Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes
Published in Nature reviews. Molecular cell biology (01-07-2016)“…Key Points Since 2007, the number of high-resolution studies of seven transmembrane domain (7TM) receptors (including G protein-coupled receptors) has greatly…”
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5
Structural and dynamic changes in P-Rex1 upon activation by PIP3 and inhibition by IP4
Published in eLife (31-07-2024)“…PIP 3 -dependent Rac exchanger 1 (P-Rex1) is abundantly expressed in neutrophils and plays central roles in chemotaxis and cancer metastasis by serving as a…”
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6
Structural insights into G protein-coupled receptor kinase function
Published in Current opinion in cell biology (01-04-2014)“…The atomic structure of a protein can greatly advance our understanding of molecular recognition and catalysis, properties of fundamental importance in signal…”
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7
Structure and function of lysosomal phospholipase A2 and lecithin:cholesterol acyltransferase
Published in Nature communications (02-03-2015)“…Lysosomal phospholipase A2 (LPLA2) and lecithin:cholesterol acyltransferase (LCAT) belong to a structurally uncharacterized family of key lipid-metabolizing…”
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Monomeric Rhodopsin Is Sufficient for Normal Rhodopsin Kinase (GRK1) Phosphorylation and Arrestin-1 Binding
Published in The Journal of biological chemistry (14-01-2011)“…G-protein-coupled receptor (GPCR) oligomerization has been observed in a wide variety of experimental contexts, but the functional significance of this…”
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9
Structural and Functional Analysis of the Regulator of G Protein Signaling 2-Gαq Complex
Published in Structure (London) (05-03-2013)“…The heterotrimeric G protein Gαq is a key regulator of blood pressure, and excess Gαq signaling leads to hypertension. A specific inhibitor of Gαq is the…”
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10
Molecular Mechanism for Inhibition of G Protein-Coupled Receptor Kinase 2 by a Selective RNA Aptamer
Published in Structure (London) (08-08-2012)“…Cardiovascular homeostasis is maintained in part by the rapid desensitization of activated heptahelical receptors that have been phosphorylated by…”
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Structures of Rhodopsin Kinase in Different Ligand States Reveal Key Elements Involved in G Protein-coupled Receptor Kinase Activation
Published in The Journal of biological chemistry (16-05-2008)“…G protein-coupled receptor (GPCR) kinases (GRKs) phosphorylate activated heptahelical receptors, leading to their uncoupling from G proteins. Here we report…”
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12
Structural Determinants of RhoA Binding and Nucleotide Exchange in Leukemia-associated Rho Guanine-Nucleotide Exchange Factor
Published in The Journal of biological chemistry (05-11-2004)“…Rho guanine-nucleotide exchange factors (RhoGEFs) activate Rho GTPases, and thereby regulate cytoskeletal structure, gene transcription, and cell migration…”
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13
Synthesis of deuterium‐labelled amlexanox and its metabolic stability against mouse, rat, and human microsomes
Published in Journal of labelled compounds & radiopharmaceuticals (15-05-2019)“…As part of a program toward making analogues of amlexanox (1), currently under clinical investigation for the treatment of type 2 diabetes and obesity, we have…”
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14
The Structure of G Protein-coupled Receptor Kinase (GRK)-6 Defines a Second Lineage of GRKs
Published in The Journal of biological chemistry (16-06-2006)“…We describe the 2.6-Å crystal structure of human G protein-coupled receptor kinase (GRK)-6, a key regulator of dopaminergic signaling and lymphocyte…”
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15
Substrate-Induced Changes in the Dynamics of Rhodopsin Kinase (G Protein-Coupled Receptor Kinase 1)
Published in Biochemistry (Easton) (24-04-2012)“…G protein-coupled receptor (GPCR) kinases (GRKs) instigate the desensitization of activated GPCRs via phosphorylation that promotes interaction with arrestins,…”
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16
New Therapeutics Targeting Heart Failure: Development of GRK2 Selective Inhibitors
Published in The FASEB journal (01-04-2012)“…Abstract only Heart failure is a leading cause of death in adults throughout the world. One of the defining characteristics of heart failure is dysregulation…”
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17
Structural analysis of thermostabilizing mutations of cocaine esterase
Published in Protein engineering, design and selection (01-07-2010)“…Cocaine is considered to be the most addictive of all substances of abuse and mediates its effects by inhibiting monoamine transporters, primarily the dopamine…”
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Paroxetine-Mediated GRK2 Inhibition Reverses Cardiac Dysfunction and Remodeling After Myocardial Infarction
Published in Journal of cardiac failure (01-08-2015)Get full text
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19
Structure of an activated G protein‐coupled receptor kinase reveals its receptor‐docking domain
Published in The FASEB journal (01-04-2009)“…Abstract only…”
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Heterotrimeric G protein β 1 γ 2 subunits change orientation upon complex formation with G protein-coupled receptor kinase 2 (GRK2) on a model membrane
Published in Proceedings of the National Academy of Sciences - PNAS (13-09-2011)“…Few experimental techniques can assess the orientation of peripheral membrane proteins in their native environment. Sum Frequency Generation (SFG) vibrational…”
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