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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Monserrat Avila-Zozaya
Apr 21, 20233 min read
VAMP2: a crucial player in the delivery of MOR to the synapse
Transporting Protein-coupled receptors (GPCRs) to the synapse, where they are involved in neurotransmission, is a complex process...
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Inês Pinheiro
Apr 11, 20234 min read
Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon interaction with their cognate...
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Inês Pinheiro
Feb 23, 20234 min read
Glyco-sulfo hotspots in the chemokine receptor system
Glycosylation and sulfation – N-terminal PTMs on chemokine receptors The interaction of chemokine receptors with their cognate chemokine...
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Inês Pinheiro
Jan 13, 20234 min read
Odorant receptors – a bit of smell for drug discovery
Odorant receptors function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR) family and...
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Inês Pinheiro
Dec 6, 20223 min read
Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery
Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors (GPCRs) can form biologically...
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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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