Stéphane A. Laporte
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View article: Development of a genetically encoded melanocortin sensor for high sensitivity in vivo imaging
Development of a genetically encoded melanocortin sensor for high sensitivity in vivo imaging Open
View article: Tunable Bias Signaling of the Angiotensin II Type 1 Receptor for Inotropy via C-Terminal Peptide Modifications and Allosteric Site Targeting
Tunable Bias Signaling of the Angiotensin II Type 1 Receptor for Inotropy via C-Terminal Peptide Modifications and Allosteric Site Targeting Open
The angiotensin II (AngII) type 1 receptor (AT1R) is a key prototypical G protein-coupled receptor in cardiovascular regulation. Biased agonists that activate G protein or β-arrestin pathways provide promising therapeutic potential, but th…
View article: Development of a genetically encoded melanocortin sensor for high sensitivity intravital imaging
Development of a genetically encoded melanocortin sensor for high sensitivity intravital imaging Open
The central melanocortin system, composed of peptides derived from pro-opiomelanocortin (POMC) such as the melanocyte-stimulating hormones (α-, β-, γ-MSH) and melanocortin 4 receptors (MC4R), along with the agouti-related protein (AgRP), p…
View article: Selective Azapeptide CD36 Ligand MPE-298 Regulates oxLDL-LOX-1-Mediated Inflammation and Mitochondrial Oxidative Stress in Macrophages
Selective Azapeptide CD36 Ligand MPE-298 Regulates oxLDL-LOX-1-Mediated Inflammation and Mitochondrial Oxidative Stress in Macrophages Open
Macrophage mitochondrial dysfunction, caused by oxidative stress, has been proposed as an essential event in the progression of chronic inflammation diseases, such as atherosclerosis. The cluster of differentiation-36 (CD36) and lectin-lik…
View article: Optimization of the prostaglandin F<sub>2α</sub>receptor for structural biology
Optimization of the prostaglandin F<sub>2α</sub>receptor for structural biology Open
Prostaglandin F 2ɑ (PGF 2ɑ ) is a bioactive lipid derived from arachidonic acid and is involved in many physiological and pathophysiological processes such as parturition, vascular tone regulation, glaucoma and inflammation. It acts by bin…
View article: Cannabis vaping elicits transcriptomic and metabolomic changes involved in inflammatory, oxidative stress, and cancer pathways in human bronchial epithelial cells
Cannabis vaping elicits transcriptomic and metabolomic changes involved in inflammatory, oxidative stress, and cancer pathways in human bronchial epithelial cells Open
Cannabis use is increasing worldwide amid broad acceptance and legalization. The prevalence of traditional smoking is diminishing in favor of vaping dry flower. This is the first study to provide initial evidence that cannabis aerosol cont…
View article: Optimization of the prostaglandin F2α receptor for structural biology.
Optimization of the prostaglandin F2α receptor for structural biology. Open
Prostaglandin F2ɑ (PGF2ɑ) is a bioactive lipid derived from arachidonic acid and is involved in many physiological and pathophysiological processes, such as parturition, vascular tone regulation, glaucoma and inflammation. It acts by bindi…
View article: Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system
Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system Open
View article: Unraveling allostery within the angiotensin II type 1 receptor for Gα <sub>q</sub> and β-arrestin coupling
Unraveling allostery within the angiotensin II type 1 receptor for Gα <sub>q</sub> and β-arrestin coupling Open
G protein–coupled receptors engage both G proteins and β-arrestins, and their coupling can be biased by ligands and mutations. Here, to resolve structural elements and mechanisms underlying effector coupling to the angiotensin II (AngII) t…
View article: Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity
Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity Open
View article: Allosteric modulation of GPCR-induced β-arrestin trafficking and signaling by a synthetic intrabody
Allosteric modulation of GPCR-induced β-arrestin trafficking and signaling by a synthetic intrabody Open
Agonist-induced phosphorylation of G protein-coupled receptors (GPCRs) is a primary determinant of β-arrestin (βarr) recruitment and trafficking. For several GPCRs such as the vasopressin receptor subtype 2 (V 2 R), agonist-stimulation fir…
View article: Prostaglandin F2α and angiotensin II type 1 receptors exhibit differential cognate G protein coupling regulation
Prostaglandin F2α and angiotensin II type 1 receptors exhibit differential cognate G protein coupling regulation Open
View article: Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system
Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system Open
Chemokine receptors constitute an important subfamily of G protein-coupled receptors (GPCRs), and they are critically involved in a broad range of immune response mechanisms. Ligand promiscuity among these receptors makes them an interesti…
View article: Standardized Cannabis Smoke Extract Induces Inflammation in Human Lung Fibroblasts
Standardized Cannabis Smoke Extract Induces Inflammation in Human Lung Fibroblasts Open
Cannabis (marijuana) is the most commonly used illicit product in the world and is the second most smoked plant after tobacco. There has been a rapid increase in the number of countries legalizing cannabis for both recreational and medicin…
View article: Allosteric modulation of GPCR-induced β-arrestin trafficking and signaling by a synthetic intrabody
Allosteric modulation of GPCR-induced β-arrestin trafficking and signaling by a synthetic intrabody Open
Agonist-induced phosphorylation of G protein-coupled receptors (GPCRs) is a primary determinant of β-arrestin (βarr) recruitment and trafficking. For several GPCRs, such as the vasopressin type II receptor (V 2 R), which exhibit high affin…
View article: Intrinsic bias at non-canonical, β-arrestin-coupled seven transmembrane receptors
Intrinsic bias at non-canonical, β-arrestin-coupled seven transmembrane receptors Open
View article: Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D2 Dopamine Receptor
Pharmacological Characterization of the Imipridone Anticancer Drug ONC201 Reveals a Negative Allosteric Mechanism of Action at the D2 Dopamine Receptor Open
View article: Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen Open
View article: Decoding Angiotensin II Type 1 Receptor Allosteric Communication to Gq and β-arrestin
Decoding Angiotensin II Type 1 Receptor Allosteric Communication to Gq and β-arrestin Open
The allosteric communication between the agonist binding site and the G protein or β-arrestin coupling sites in G protein-coupled receptors (GPCRs) play an important role in determining ligand efficacy towards these two signaling pathways …
View article: Intrinsic bias at non-canonical, β-arrestin-coupled seven transmembrane receptors
Intrinsic bias at non-canonical, β-arrestin-coupled seven transmembrane receptors Open
G protein-coupled receptors (GPCRs) are typically characterized by their seven transmembrane (7TM) architecture, and interaction with two universal signal-transducers namely, the heterotrimeric G-proteins and β-arrestins (βarrs). Synthetic…
View article: Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen Open
Internalization and intracellular trafficking of hormone receptors, like receptor tyrosine kinases (RTKs) and G protein-coupled receptors (GPCRs), play pivotal roles in cell responsiveness homeostasis. Dysregulation in receptor trafficking…
View article: Key phosphorylation sites in <scp>GPCR</scp> s orchestrate the contribution of β‐Arrestin 1 in <scp>ERK</scp> 1/2 activation
Key phosphorylation sites in <span>GPCR</span> s orchestrate the contribution of β‐Arrestin 1 in <span>ERK</span> 1/2 activation Open
View article: Angiotensin II type 1 receptor variants alter endosomal receptor–β-arrestin complex stability and MAPK activation
Angiotensin II type 1 receptor variants alter endosomal receptor–β-arrestin complex stability and MAPK activation Open
View article: Signal profiling of the β1AR reveals coupling to novel signalling pathways and distinct phenotypic responses mediated by β1AR and β2AR
Signal profiling of the β1AR reveals coupling to novel signalling pathways and distinct phenotypic responses mediated by β1AR and β2AR Open
View article: Genetic code expansion and photocross-linking identify different β-arrestin binding modes to the angiotensin II type 1 receptor
Genetic code expansion and photocross-linking identify different β-arrestin binding modes to the angiotensin II type 1 receptor Open
The angiotensin II (AngII) type 1 receptor (AT1R) is a member of the G protein-coupled receptor (GPCR) family and binds β-arrestins (β-arrs), which regulate AT1R signaling and trafficking. These processes can be biased by different ligands…
View article: Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9
Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9 Open
β-Arrestin proteins fine-tune different GPCR-stimulated pathways that converge on ERK1/2 activation.
View article: Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor
Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor Open
The dopamine D2 receptor (D2R) is known to elicit effects through activating two major signaling pathways mediated by either G proteins (Gi/o) or β-arrestins. However, the specific role of each pathway in physiological or therapeutic activ…
View article: A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling
A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling Open
View article: Oncogenic effects of urotensin-II in cells lacking tuberous sclerosis complex-2
Oncogenic effects of urotensin-II in cells lacking tuberous sclerosis complex-2 Open
Lymphangioleiomyomatosis (LAM) is a destructive lung disease that can arise sporadically or in adults suffering from the tumor syndrome tuberous sclerosis complex (TSC). Microscopic tumors ('LAM nodules') in the lung interstitium arise fro…
View article: Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET
Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET Open