Search Results - "Boldizsar, Noelia"
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G protein‐coupled receptor kinases regulate &[beta]‐arrestin interactions with the D2 dopamine receptor in an isoform‐specific manner and in the absence of direct receptor phosphorylation
Published in The FASEB journal (01-05-2022)“…The D2 dopamine receptor (D2R) regulates numerous CNS functions including movement, cognition, emotion, and reward circuitry. Agonist binding to the D2R…”
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2
Location bias contributes to functionally selective responses of biased CXCR3 agonists
Published in Nature communications (04-10-2022)“…Some G protein-coupled receptor (GPCR) ligands act as “biased agonists” that preferentially activate specific signaling transducers over others. Although GPCRs…”
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3
G Protein-Coupled Receptor Kinase 2 Selectively Enhances β-Arrestin Recruitment to the D2 Dopamine Receptor through Mechanisms That Are Independent of Receptor Phosphorylation
Published in Biomolecules (Basel, Switzerland) (20-10-2023)“…The D2 dopamine receptor (D2R) signals through both G proteins and β-arrestins to regulate important physiological processes, such as movement, reward…”
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Identification and Characterization of ML321: A Novel and Highly Selective D2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity
Published in ACS pharmacology & translational science (13-01-2023)“…We have developed and characterized a novel D2R antagonist with exceptional GPCR selectivity – ML321. In functional profiling screens of 168 different GPCRs,…”
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Identification and Characterization of ML321: A Novel and Highly Selective D 2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical Antipsychotic Activity
Published in ACS pharmacology & translational science (13-01-2023)“…We have developed and characterized a novel D2R antagonist with exceptional GPCR selectivity - ML321. In functional profiling screens of 168 different GPCRs,…”
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6
Biased agonism at chemokine receptors
Published in Cellular signalling (01-02-2021)“…In the human chemokine system, interactions between the approximately 50 known endogenous chemokine ligands and 20 known chemokine receptors (CKRs) regulate a…”
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Sympathetic and Parasympathetic Regulation of NF‐κB by GPCRs through the modulation of interactions between p65/RelA and the β‐arrestins
Published in The FASEB journal (01-05-2021)“…Study Objective: This project sought to elucidate the biological mechanisms and physiological significance of β2 adrenergic receptor (B2AR)‐ and M1 muscarinic…”
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8
Receptor Endocytosis as a Mechanism of Biased Agonism at CXCR3
Published in The FASEB journal (01-05-2021)“…G Protein Coupled Receptors (GPCRs) are the largest class of receptors in the human genome. They are expressed in virtually every cell type and are implicated…”
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9
Differential GRK Recruitment and the Phosphorylation Barcode as a Mechanism for Biased Agonism at G Protein‐Coupled Receptors
Published in The FASEB journal (01-05-2021)“…G Protein‐Coupled Receptors (GPCRs) are the largest and most diverse family of cell receptors in the human genome and account for ~30% of all FDA‐approved…”
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10
Location Bias of G Protein‐Coupled Receptor Kinases Promotes Biased Signaling at CXCR3
Published in The FASEB journal (01-05-2022)“…G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors and are known to canonically signal through two main effector proteins: G…”
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11
Location Bias Contributes to Functionally Selective Responses of Biased CXCR3 Agonists to Regulate Inflammation
Published in The FASEB journal (01-05-2022)“…G Protein‐Coupled Receptors (GPCRs) represent the largest and most diverse family of cell receptors in the human genome and are targeted by ~35% of all…”
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12
Phosphorylation barcodes direct biased chemokine signaling at CXCR3
Published in Cell chemical biology (20-04-2023)“…G protein-coupled receptor (GPCR)-biased agonism, selective activation of certain signaling pathways relative to others, is thought to be directed by…”
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13
Biased agonists of the chemokine receptor CXCR3 differentially signal through Gα i :β-arrestin complexes
Published in Science signaling (22-03-2022)“…G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors and signal through the proximal effectors, G proteins and β-arrestins, to…”
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Characterization and Chemical Optimization of the D2 Dopamine Receptor‐Selective Antagonist, ML321, Identifies Lead Compounds for the Clinical Treatment of Neuropsychiatric Disorders
Published in The FASEB journal (01-05-2022)“…Schizophrenia is a devastating illness characterized by both positive (hallucinations, delusions) and negative (flat affect, decreased motivation) symptoms…”
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15
Phosphorylation barcode ensembles encoded by biased CXCR3 agonists direct non‐redundant chemokine signaling
Published in The FASEB journal (01-05-2022)“…Chemokine receptors, a group of G protein‐coupled receptors (GPCRs), interact with transducers such as G proteins, β‐arrestins, and GPCR kinases (GRKs). In the…”
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Novel Dopamine D4 Receptor‐Selective Antagonists For Neuropsychiatric Disorders
Published in The FASEB journal (01-05-2022)“…The neurotransmitter dopamine signals through G protein‐coupled receptors that regulate a variety of neurophysiological functions, including movement,…”
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Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder
Published in Journal of medicinal chemistry (14-09-2023)“…Pharmacological targeting of the dopamine D4 receptor (D4R)expressed in brain regions that control cognition, attention, and decision-makingcould be useful…”
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18
G Protein-Coupled Receptor Kinase 2 Selectively Enhances beta-Arrestin Recruitment to the D[sub.2] Dopamine Receptor through Mechanisms That Are Independent of Receptor Phosphorylation
Published in Biomolecules (Basel, Switzerland) (01-10-2023)“…The D2 dopamine receptor (D2R) signals through both G proteins and β-arrestins to regulate important physiological processes, such as movement, reward…”
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Journal Article -
19
G Protein-Coupled Receptor Kinase 2 Selectively Enhances β-Arrestin Recruitment to the D 2 Dopamine Receptor through Mechanisms That Are Independent of Receptor Phosphorylation
Published in Biomolecules (Basel, Switzerland) (20-10-2023)“…The D2 dopamine receptor (D2R) signals through both G proteins and β-arrestins to regulate important physiological processes, such as movement, reward…”
Get full text
Journal Article