Targeting Intracellular Allosteric Sites in GPCRs
Exploring the intracellular allosteric site GPCRs represent one of the largest and most vital families of cell surface receptors, playing...
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Inês Pinheiro
Aug 21, 20235 min read
Decoding β-Arrestins: from Structure to function
Fine-tuning GPCR signaling: conformational dynamics and intracellular responses GPCR signaling is a complex process modulated by protein...
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Inês Pinheiro
Jun 28, 20237 min read
Structural landscape of the Chemokine Receptor system
Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial role in inflammation and...
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Inês Pinheiro
May 16, 20235 min read
Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
Artificial intelligence - Machine learning vs Deep Learning GPCRs have long been recognized as important drug targets, and numerous drugs...
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GPCR News
Oct 31, 20221 min read
Emerging approaches for decoding neuropeptide transmission
November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in...
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GPCR News
Oct 31, 20221 min read
Location bias contributes to functionally selective responses of biased CXCR3 agonists
November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially activate specific signaling...
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GPCR News
Oct 31, 20221 min read
Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis...
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GPCR News
Oct 31, 20221 min read
Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding...
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GPCR News
Oct 31, 20221 min read
Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling
November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies. A hallmark of aGPCR...
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GPCR News
Oct 31, 20221 min read
Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors
November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures have been cocrystallized...
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GPCR News
Oct 31, 20221 min read
Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inv
November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies. However, the function of...
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GPCR News
Sep 30, 20221 min read
High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR...
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GPCR News
Sep 30, 20221 min read
Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex
October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation and to initiate key signaling...
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GPCR News
Sep 30, 20221 min read
Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias...
October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the...
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GPCR News
Sep 30, 20221 min read
Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical seven transmembrane (TM) helix...
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GPCR News
Sep 30, 20221 min read
Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to...
October 2022 Increased Anxiety-like Behaviors in Adgra1-/- Male But Not Female Mice are Attributable to Elevated Neuron Dendrite Density,...
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GPCR News
Sep 30, 20221 min read
Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to...
October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inverse agonism...
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GPCR News
Sep 30, 20221 min read
Structural view of G protein-coupled receptor signaling in the retinal rod outer segment
October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR) signaling pathway because of its...
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GPCR News
Sep 30, 20221 min read
Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy...
October 2022 Case Report of a Juvenile Patient with Autism Spectrum Disorder with a Novel Combination of Copy Number Variants in ADGRL3...
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GPCR News
Sep 30, 20221 min read
Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine..
October 2022 Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for...
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