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Human Gain-of-Function MC4R Variants Show Signaling Bias and Protect against Obesity

Cell, 2019-04, Vol.177 (3), p.597-607.e9

2019

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Loss-of-function mutations in the melanocortin 4 receptor in a UK birth cohort

Nature medicine, 2021-06, Vol.27 (6), p.1088-1096

2021

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Human MC4R variants affect endocytosis, trafficking and dimerization revealing multiple cellular mechanisms involved in weight regulation

Cell reports (Cambridge), 2021-03, Vol.34 (12), p.108862-108862, Article 108862

2021

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Obesity-Associated GNAS Mutations and the Melanocortin Pathway

The New England journal of medicine, 2021-10, Vol.385 (17), p.1581-1592

2021

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A rare human variant that disrupts GPR10 signalling causes weight gain in mice

Nature communications, 2023-03, Vol.14 (1), p.1450-1450, Article 1450

2023

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Modulation of Constitutive Activity and Signaling Bias of the Ghrelin Receptor by Conformational Constraint in the Second Extracellular Loop

The Journal of biological chemistry, 2012-09, Vol.287 (40), p.33488-33502

2012

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Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency

Molecular metabolism (Germany), 2017-10, Vol.6 (10), p.1321-1329

2017

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Modulation of the Constitutive Activity of the Ghrelin Receptor by Use of Pharmacological Tools and Mutagenesis

Constitutive Activity in Receptors and Other Proteins, Part A, 2010, Vol.484, p.53-73

2010

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The Location of Missense Variants in the Human GIP Gene Is Indicative for Natural Selection

Frontiers in endocrinology (Lausanne), 2022-06, Vol.13, p.891586-891586

2022

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The E92K melanocortin 1 receptor mutant induces cAMP production and arrestin recruitment but not ERK activity indicating biased constitutive signaling

PloS one, 2011-09, Vol.6 (9), p.e24644

2011

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Overlapping Binding Site for the Endogenous Agonist, Small-Molecule Agonists, and Ago-allosteric Modulators on the Ghrelin Receptor

Molecular pharmacology, 2009-01, Vol.75 (1), p.44-59

2009

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Identification of an Efficacy Switch Region in the Ghrelin Receptor Responsible for Interchange between Agonism and Inverse Agonism

The Journal of biological chemistry, 2007-05, Vol.282 (21), p.15799-15811

2007

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The GLP-1R as a model for understanding and exploiting biased agonism in next-generation medicines

Journal of endocrinology, 2024-05, Vol.261 (2)

2024

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Expression of Endoglin in Primary Endometrial Cancer

Oncology, 2011-01, Vol.81 (3-4), p.243-250

2011

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MC4R agonism promotes durable weight loss in patients with leptin receptor deficiency

Nature Medicine, 2018-05, Vol.24 (5), p.551-555

2018

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Palmitic Acid Hydroxystearic Acids Activate GPR40, Which Is Involved in Their Beneficial Effects on Glucose Homeostasis

Cell metabolism, 2018-02, Vol.27 (2), p.419-427.e4

2018

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TGF beta signalling accessory receptors

Postępy biochemii, 2008, Vol.54 (3), p.264

2008

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Human loss-of-function variants in the serotonin 2C receptor associated with obesity and maladaptive behavior

Nature medicine, 2022-12, Vol.28 (12), p.2537-2546

2022

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Biased Gs versus Gq proteins and β-arrestin signaling in the NK1 receptor determined by interactions in the water hydrogen bond network

The Journal of biological chemistry, 2015-10, Vol.290 (40), p.24495-24508

2015

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The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW

Neurochemistry international, 2017-01, Vol.102, p.105-113

2017

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Biased GsVersus Gq Proteins and β-Arrestin Signaling in the NK1 Receptor Determined by Interactions in the Water Hydrogen Bond Network

The Journal of biological chemistry, 2015-10, Vol.290 (40), p.24495-24508

2015

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Allosteric and Orthosteric Sites in CC Chemokine Receptor (CCR5), a Chimeric Receptor Approach

The Journal of biological chemistry, 2011-10, Vol.286 (43), p.37543-37554

2011

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Conserved Water-mediated Hydrogen Bond Network between TM-I, -II, -VI, and -VII in 7TM Receptor Activation

The Journal of biological chemistry, 2010-06, Vol.285 (25), p.19625-19636

2010

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The aromatic amino acid sensor GPR142 controls metabolism through balanced regulation of pancreatic and gut hormones

Molecular metabolism (Germany), 2019-01, Vol.19, p.49-64

2019

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Human Gain-of-Function MC4R Variants Show Signaling Bias and Protect against Obesity

Loss-of-function mutations in the melanocortin 4 receptor in a UK birth cohort

Human MC4R variants affect endocytosis, trafficking and dimerization revealing multiple cellular mechanisms involved in weight regulation

Obesity-Associated GNAS Mutations and the Melanocortin Pathway

A rare human variant that disrupts GPR10 signalling causes weight gain in mice

Characterization of genetic variants of GIPR reveals a contribution of β-arrestin to metabolic phenotypes

Modulation of Constitutive Activity and Signaling Bias of the Ghrelin Receptor by Conformational Constraint in the Second Extracellular Loop

Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency

Modulation of the Constitutive Activity of the Ghrelin Receptor by Use of Pharmacological Tools and Mutagenesis

The Location of Missense Variants in the Human GIP Gene Is Indicative for Natural Selection

The E92K melanocortin 1 receptor mutant induces cAMP production and arrestin recruitment but not ERK activity indicating biased constitutive signaling

Overlapping Binding Site for the Endogenous Agonist, Small-Molecule Agonists, and Ago-allosteric Modulators on the Ghrelin Receptor

Identification of an Efficacy Switch Region in the Ghrelin Receptor Responsible for Interchange between Agonism and Inverse Agonism

The GLP-1R as a model for understanding and exploiting biased agonism in next-generation medicines

Expression of Endoglin in Primary Endometrial Cancer

MC4R agonism promotes durable weight loss in patients with leptin receptor deficiency

Palmitic Acid Hydroxystearic Acids Activate GPR40, Which Is Involved in Their Beneficial Effects on Glucose Homeostasis

TGF beta signalling accessory receptors

Human loss-of-function variants in the serotonin 2C receptor associated with obesity and maladaptive behavior

Biased Gs versus Gq proteins and β-arrestin signaling in the NK1 receptor determined by interactions in the water hydrogen bond network

The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW

Biased GsVersus Gq Proteins and β-Arrestin Signaling in the NK1 Receptor Determined by Interactions in the Water Hydrogen Bond Network

Allosteric and Orthosteric Sites in CC Chemokine Receptor (CCR5), a Chimeric Receptor Approach

Conserved Water-mediated Hydrogen Bond Network between TM-I, -II, -VI, and -VII in 7TM Receptor Activation

The aromatic amino acid sensor GPR142 controls metabolism through balanced regulation of pancreatic and gut hormones

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