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List of works by Mette M. Rosenkilde

2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans

scientific article (publication date: September 2011)

A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus.

scientific article published on September 1997

A highly conserved glycine within linker I and the extreme C terminus of G protein alpha subunits interact cooperatively in switching G protein-coupled receptor-to-effector specificity

scientific article published on 22 December 2004

AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor

scientific article published on September 2005

Activation of the CXCR3 chemokine receptor through anchoring of a small molecule chelator ligand between TM-III, -IV, and -VI

scientific article published on 14 December 2006

Agonists and inverse agonists for the herpesvirus 8-encoded constitutively active seven-transmembrane oncogene product, ORF-74

scientific article

Allosteric and orthosteric sites in CC chemokine receptor (CCR5), a chimeric receptor approach

scientific article published on 30 August 2011

An atlas of O-linked glycosylation on peptide hormones reveals diverse biological roles

scientific article published on 20 August 2020

Arrestin-independent constitutive endocytosis of GPR125/ADGRA3

scientific article published on 29 October 2019

Attenuation of chemokine receptor function and surface expression as an immunomodulatory strategy employed by human cytomegalovirus is linked to vGPCR US28.

scientific article published on 12 December 2016

Autocrine CCL19 blocks dendritic cell migration toward weak gradients of CCL21.

scientific article published on 13 July 2016

Biased Signaling of CCL21 and CCL19 Does Not Rely on N-Terminal Differences, but Markedly on the Chemokine Core Domains and Extracellular Loop 2 of CCR7

scientific article published on 13 September 2019

Biased agonism and allosteric modulation of G protein-coupled receptor 183 - a 7TM receptor also known as Epstein-Barr virus-induced gene 2.

scientific article

Biased and constitutive signaling in the CC-chemokine receptor CCR5 by manipulating the interface between transmembrane helices 6 and 7.

scientific article published on 14 March 2013

Biased and g protein-independent signaling of chemokine receptors

scientific article

Biased signaling of G protein-coupled receptors - From a chemokine receptor CCR7 perspective

scientific article

Biased signaling of lipids and allosteric actions of synthetic molecules for GPR119.

scientific article published on 25 August 2016

Biased small-molecule ligands for selective inhibition of HIV-1 cell entry via CCR5.

scientific article published on 18 October 2016

Bile acids are important direct and indirect regulators of the secretion of appetite- and metabolism-regulating hormones from the gut and pancreas

scientific article published on 17 March 2018

CCL19 with CCL21-tail displays enhanced glycosaminoglycan binding with retained chemotactic potency in dendritic cells

scientific article published on 16 May 2018

CD4-Chemokine receptor hybrids in human immunodeficiency virus type 1 infection.

scientific article published on September 1999

Cell transformation mediated by the Epstein-Barr virus G protein-coupled receptor BILF1 is dependent on constitutive signaling.

scientific article published on 14 June 2010

Chapter 8. Activation mechanisms of chemokine receptors

scientific article published in January 2009

Circulating Glucagon 1-61 Regulates Blood Glucose by Increasing Insulin Secretion and Hepatic Glucose Production

scientific article published in November 2017

Comparing olive oil and C4-dietary oil, a prodrug for the GPR119 agonist, 2-oleoyl glycerol, less energy intake of the latter is needed to stimulate incretin hormone secretion in overweight subjects with type 2 diabetes

scientific article published on 12 January 2018

Conformational constraining of inactive and active States of a seven transmembrane receptor by metal ion site engineering in the extracellular end of transmembrane segment V.

scientific article published on 13 September 2006

Corrigendum: Differential CCR7 Targeting in Dendritic Cells by Three Naturally Occurring CC-Chemokines

scientific article published on 8 February 2017

Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4).

scientific article published on 14 July 2014

Determination of the binding mode for the cyclopentapeptide CXCR4 antagonist FC131 using a dual approach of ligand modifications and receptor mutagenesis

scientific article published on December 2014

Development of highly efficient protocols for extraction and amplification of cytomegalovirus DNA from dried blood spots for detection and genotyping of polymorphic immunomodulatory genes

scientific article published on 12 September 2019

Development of potent and proteolytically stable human neuromedin U receptor agonists.

scientific article published on 14 December 2017

Differential CCR7 Targeting in Dendritic Cells by Three Naturally Occurring CC-Chemokines

scientific article published on 09 December 2016

Discovery and Characterization of Biased Allosteric Agonists of the Chemokine Receptor CXCR3

article

Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2.

scientific article

Distinct Roles of Extracellular Domains in the Epstein-Barr Virus-Encoded BILF1 Receptor for Signaling and Major Histocompatibility Complex Class I Downregulation

scientific article published on 15 January 2019

Distinct expression and ligand-binding profiles of two constitutively active GPR17 splice variants.

scientific article published on 8 February 2010

Dual treatment with a fixed ratio of glucagon and insulin increases the therapeutic window of insulin in diabetic rats.

scientific article published in March 2018

EBI2 overexpression in mice leads to B1 B-cell expansion and chronic lymphocytic leukemia-like B-cell malignancies

scientific article published on 21 December 2016

EBI2, GPR18 and GPR17--three structurally related, but biologically distinct 7TM receptors

scientific article published on January 2011

EBV, the human host, and the 7TM receptors: defense or offense?

scientific article

Effect of Intracoronary and Intravenous Melatonin on Myocardial Salvage Index in Patients with ST-Elevation Myocardial Infarction: a Randomized Placebo Controlled Trial

scientific article

Enhanced agonist residence time, internalization rate and signalling of the GIP receptor variant [E354Q] facilitate receptor desensitization and long-term impairment of the GIP system

scientific article published on 12 July 2019

Epstein-Barr virus-encoded BILF1 is a constitutively active G protein-coupled receptor

scientific article

Evaluation of the incretin effect in humans using GIP and GLP-1 receptor antagonists

scientific article published on 03 November 2019

Exendin-4, but not dipeptidyl peptidase IV inhibition, increases small intestinal mass in GK rats

scientific article published on 12 April 2007

Extracellular disulfide bridges serve different purposes in two homologous chemokine receptors, CCR1 and CCR5.

scientific article published on 13 June 2013

Functional analysis of the murine cytomegalovirus chemokine receptor homologue M33: ablation of constitutive signaling is associated with an attenuated phenotype in vivo

scientific article

G Protein-Coupled Receptors in the Sweet Spot: Glycosylation and other Post-translational Modifications

scientific article published on 17 March 2020

GIP's effect on bone metabolism is reduced by the selective GIP receptor antagonist GIP(3-30)NH2

scientific article published on 14 October 2019

GIP(3-30)NH2 is a potent competitive antagonist of the GIP receptor and effectively inhibits GIP-mediated insulin, glucagon, and somatostatin release.

scientific article published on 22 February 2017

GIP(3-30)NH2 is an efficacious GIP receptor antagonist in humans: a randomised, double-blinded, placebo-controlled, crossover study

scientific article

GIP-(3–42) does not antagonize insulinotropic effects of GIP at physiological concentrations

scientific article published on 11 April 2006

GLP-1 Val8: A Biased GLP-1R Agonist with Altered Binding Kinetics and Impaired Release of Pancreatic Hormones in Rats

scientific article published on 19 January 2021

GLP-2 and GIP exert separate effects on bone turnover: A randomized, placebo-controlled, crossover study in healthy young men

scientific article published on 15 May 2019

GPR119 as a fat sensor

scientific article published on 02 May 2012

GPR183 Is Dispensable for B1 Cell Accumulation and Function, but Affects B2 Cell Abundance, in the Omentum and Peritoneal Cavity

scientific article published on 31 January 2022

Gating function of isoleucine-116 in TM-3 (position III:16/3.40) for the activity state of the CC-chemokine receptor 5 (CCR5).

scientific article

GluVII:06--a highly conserved and selective anchor point for non-peptide ligands in chemokine receptors

scientific article published on January 2006

Glucagon-like peptide-1 (GLP-1) receptor agonism or DPP-4 inhibition does not accelerate neoplasia in carcinogen treated mice

scientific article published on 15 September 2012

Glucose and amino acid metabolism in mice depend mutually on glucagon and insulin receptor signaling

scientific article published on 26 February 2019

Glucose-dependent insulinotropic polypeptide (GIP) receptor antagonists as anti-diabetic agents

scientific article published in February 2018

Glucose-dependent insulinotropic polypeptide augments glucagon responses to hypoglycemia in type 1 diabetes

scientific article published on 22 July 2014

Glucose-lowering effects and mechanisms of the bile acid-sequestering resin sevelamer

scientific article published in March 2018

High constitutive activity of a virus-encoded seven transmembrane receptor in the absence of the conserved DRY motif (Asp-Arg-Tyr) in transmembrane helix 3.

scientific article

High content screening for G protein-coupled receptors using cell-based protein translocation assays

scientific article published in June 2005

Homozygous carriers of the G allele of rs4664447 of the glucagon gene (GCG) are characterised by decreased fasting and stimulated levels of insulin, glucagon and glucagon-like peptide (GLP)-1.

scientific article published on 7 August 2011

How receptor mutagenesis may confirm or confuse receptor classification.

scientific article published on May 1997

Human GIP(3-30)NH2 inhibits G protein-dependent as well as G protein-independent signaling and is selective for the GIP receptor with high-affinity binding to primate but not rodent GIP receptors

scientific article published on 25 January 2018

Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor

scientific journal article

Identification and functional comparison of seven-transmembrane G-protein-coupled BILF1 receptors in recently discovered nonhuman primate lymphocryptoviruses

scientific article

Identification of a novel site within G protein alpha subunits important for specificity of receptor-G protein interaction

scientific article

Identification of common mechanisms by which human and mouse cytomegalovirus seven-transmembrane receptor homologues contribute to in vivo phenotypes in a mouse model

scientific article (publication date: April 2013)

In vivo and in vitro degradation of peptide YY3-36 to inactive peptide YY3-34 in humans

scientific article published on 27 January 2016

Increased Body Weight and Fat Mass After Subchronic GIP Receptor Antagonist, but Not GLP-2 Receptor Antagonist, Administration in Rats

scientific article published on 06 August 2019

Influence of chain length on the activity of tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4).

scientific article published on 21 November 2016

Inhibition of HIV fusion by small molecule agonists through efficacy-engineering of CXCR4.

scientific article published on 20 February 2018

Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist

scientific article published on December 2004

Interaction of chemokines with their receptors--from initial chemokine binding to receptor activating steps

scientific article

International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors

scientific article

Kaposi sarcoma-associated herpes virus targets the lymphotactin receptor with both a broad spectrum antagonist vCCL2 and a highly selective and potent agonist vCCL3

scientific article

Ligand binding and micro-switches in 7TM receptor structures

scientific article published on 16 April 2009

Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: identification of a potent and efficacious inverse agonist

scientific article

Ligand-selective small molecule modulators of the constitutively active vGPCR US28

scientific article published on 31 May 2018

Maintenance of improvements in fitness and fatness 1 year after a 3-month lifestyle intervention in overweight men

scientific article published on 20 April 2016

Metal ion enhanced binding of AMD3100 to Asp262 in the CXCR4 receptor

scientific article published in January 2003

Microbiological exploitation of the chemokine system

scientific article

Modest human immunodeficiency virus coreceptor function of CXCR3 is strongly enhanced by mimicking the CXCR4 ligand binding pocket in the CXCR3 receptor

scientific article published on 24 January 2007

Modulation in Selectivity and Allosteric Properties of Small-Molecule Ligands for CC-Chemokine Receptors

Molecular Mechanism of Action for Allosteric Modulators and Agonists in CC-chemokine Receptor 5 (CCR5).

scientific article published on 10 November 2016

Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183)

scientific journal article

Molecular interaction of a potent nonpeptide agonist with the chemokine receptor CCR8

scientific article published on 01 August 2007

Molecular interactions of full-length and truncated GIP peptides with the GIP receptor - A comprehensive review

scientific article published on 03 December 2019

Molecular mechanism of 7TM receptor activation--a global toggle switch model

scientific article

Molecular mechanism of AMD3100 antagonism in the CXCR4 receptor: transfer of binding site to the CXCR3 receptor

scientific article published on 28 October 2003

Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor

scientific article

Molecular pharmacological phenotyping of EBI2. An orphan seven-transmembrane receptor with constitutive activity

scientific article

Molecular requirements for inhibition of the chemokine receptor CCR8--probe-dependent allosteric interactions.

scientific article

Multistep continuous-flow synthesis in medicinal chemistry: discovery and preliminary structure-activity relationships of CCR8 ligands

scientific article published on 28 May 2013

Mutational analysis of CCL20 reveals flexibility of N-terminal amino acid composition and length

scientific article published on 01 August 2018

Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding.

scientific article published on November 1994

Mutations at the CXCR4 interaction sites for AMD3100 influence anti-CXCR4 antibody binding and HIV-1 entry

scientific article published in July 2003

N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor

scientific article published on 17 November 2015

Natural agonist enhancing bis-His zinc-site in transmembrane segment V of the tachykinin NK3 receptor

scientific article published on 01 November 1998

Natural nitration of CXCL12 reduces its signaling capacity and chemotactic activity in vitro and abrogates intra-articular lymphocyte recruitment in vivo.

scientific article published on 23 August 2016

Neuromedin U Does Not Act as a Decretin in Rats

scientific article published on 15 November 2018

Novel Chemokine-Based Immunotoxins for Potent and Selective Targeting of Cytomegalovirus Infected Cells.

scientific article published on 30 January 2017

Oleoyl-lysophosphatidylinositol enhances glucagon-like peptide-1 secretion from enteroendocrine L-cells through GPR119

scientific article published on 05 June 2018

Oral 2-oleyl glyceryl ether improves glucose tolerance in mice through the GPR119 receptor.

scientific article published on 14 June 2016

Oxyntomodulin: Actions and role in diabetes

scientific article published in February 2018

Oxysterol-EBI2 signaling in immune regulation and viral infection

scientific article published on 20 June 2014

Paracrine crosstalk between intestinal L- and D-cells controls secretion of glucagon-like peptide-1 in mice

scientific article published on 10 September 2019

Partial functional complementation between human and mouse cytomegalovirus chemokine receptor homologues

scientific article

Peroxynitrite Exposure of CXCL12 Impairs Monocyte, Lymphocyte and Endothelial Cell Chemotaxis, Lymphocyte Extravasation and Anti-HIV-1 Activity

article

Perspective: Implications of Ligand-Receptor Binding Kinetics for Therapeutic Targeting of G Protein-Coupled Receptors

scientific article published on 18 March 2020

Pharmacokinetics of high-dose intravenous melatonin in humans

scientific article published on 14 September 2015

Pharmacokinetics of oral and intravenous melatonin in healthy volunteers

scientific article published on 19 February 2016

Phorbol esters and SDF-1 induce rapid endocytosis and down modulation of the chemokine receptor CXCR4.

scientific article

Physiology of the Incretin Hormones, GIP and GLP-1-Regulation of Release and Posttranslational Modifications

scientific article published on 19 September 2019

Porcine glucagon-like peptide-2: structure, signaling, metabolism and effects

scientific article published on 28 November 2007

Positive versus negative modulation of different endogenous chemokines for CC-chemokine receptor 1 by small molecule agonists through allosteric versus orthosteric binding

scientific article published on 17 June 2008

Potency of ligands correlates with affinity measured against agonist and inverse agonists but not against neutral ligand in constitutively active chemokine receptor

scientific article published on 01 March 2000

Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist.

scientific article published on April 1997

Probing Biased Signaling in Chemokine Receptors

scientific article published on 14 November 2015

Probing the Molecular Interactions between CXC Chemokine Receptor 4 (CXCR4) and an Arginine-Based Tripeptidomimetic Antagonist (KRH-1636)

scientific article published on 02 October 2015

Progress toward rationally designed small-molecule peptide and peptidomimetic CXCR4 antagonists

scientific article published on July 2015

Prohormone convertase 1/3 is essential for processing of the glucose-dependent insulinotropic polypeptide precursor

scientific article published on 13 February 2006

Protein engineering of the chemokine CCL20 prevents psoriasiform dermatitis in an IL-23-dependent murine model.

scientific article published on 6 November 2017

Rat cytomegalovirus-encoded γ-chemokine vXCL1 is a highly adapted, species-specific agonist for rat XCR1-positive dendritic cells

scientific article published on 18 November 2019

Rational design of conformationally constrained cyclopentapeptide antagonists for C-x-C chemokine receptor 4 (CXCR4)

scientific article published on 22 October 2012

Rationally designed chemokine-based toxin targeting the viral G protein-coupled receptor US28 potently inhibits cytomegalovirus infection in vivo

scientific article published on 15 June 2015

Recent advances of GIP and future horizons

scientific article published on 12 December 2019

Reversed binding of a small molecule ligand in homologous chemokine receptors - differential role of extracellular loop 2.

scientific article published on May 2012

Role of Conserved Disulfide Bridges and Aromatic Residues in Extracellular Loop 2 of Chemokine Receptor CCR8 for Chemokine and Small Molecule Binding

scientific article

Selective Allosteric Modulation of N-Terminally Cleaved, but Not Full Length CCL3 in CCR1

scientific article published on 13 November 2019

Selective recognition of the membrane-bound CX3C chemokine, fractalkine, by the human cytomegalovirus-encoded broad-spectrum receptor US28

scientific article published on 01 December 1998

Separate and Combined Glucometabolic Effects of Endogenous Glucose-Dependent Insulinotropic Polypeptide and Glucagon-like Peptide 1 in Healthy Individuals

scientific article published on 09 January 2019

Signaling via G proteins mediates tumorigenic effects of GPR87.

scientific article published on 16 November 2016

Similar activation of signal transduction pathways by the herpesvirus-encoded chemokine receptors US28 and ORF74.

scientific article published on August 2004

Small molecule antagonism of oxysterol-induced Epstein-Barr virus induced gene 2 (EBI2) activation

scientific article published on 19 February 2013

Species-specific action of (Pro3)GIP - a full agonist at human GIP receptors, but a partial agonist and competitive antagonist at rat and mouse GIP receptors

scientific article published on 11 September 2015

Structural Diversity in Conserved Regions Like the DRY-Motif among Viral 7TM Receptors-A Consequence of Evolutionary Pressure?

scientific article published on 30 July 2012

Structural Features of an Extended C-Terminal Tail Modulate the Function of the Chemokine CCL21

scientific article published on 26 March 2020

Structural motifs of importance for the constitutive activity of the orphan 7TM receptor EBI2: analysis of receptor activation in the absence of an agonist

scientific journal article

Structure, function and physiological consequences of virally encoded chemokine seven transmembrane receptors

scientific article

Structure-activity relationship studies of the aromatic positions in cyclopentapeptide CXCR4 antagonists

scientific article published on 23 October 2013

Structure-activity relationships and identification of optmized CC-chemokine receptor CCR1, 5, and 8 metal-ion chelators

scientific article published on 22 October 2013

Structure-based discovery of novel US28 small molecule ligands with different modes of action

scientific article published on 29 August 2016

Structure-function guided modeling of chemokine-GPCR specificity for the chemokine XCL1 and its receptor XCR1

scientific article published on 03 September 2019

Sustained effect of glucagon on body weight and blood glucose: Assessed by continuous glucose monitoring in diabetic rats.

scientific article published on 20 March 2018

Sweet Taste Receptor Activation in the Gut Is of Limited Importance for Glucose-Stimulated GLP-1 and GIP Secretion

scientific article

Targeting herpesvirus reliance of the chemokine system

scientific article

Targeting the latent cytomegalovirus reservoir with an antiviral fusion toxin protein.

scientific article published on 02 February 2017

The CXC chemokine receptor encoded by herpesvirus saimiri, ECRF3, shows ligand-regulated signaling through Gi, Gq, and G12/13 proteins but constitutive signaling only through Gi and G12/13 proteins

scientific article published on 20 May 2004

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

scientific article

The European Research Network on Signal Transduction (ERNEST): Toward a Multidimensional Holistic Understanding of G Protein-Coupled Receptor Signaling

scientific article published on 31 March 2020

The Gluco- and Liporegulatory and Vasodilatory Effects of Glucose-Dependent Insulinotropic Polypeptide (GIP) Are Abolished by an Antagonist of the Human GIP Receptor

scientific article

The anorexic hormone Peptide YY3-36 is rapidly metabolized to inactive Peptide YY3-34 in vivo

scientific article

The carboxyl terminus of human cytomegalovirus-encoded 7 transmembrane receptor US28 camouflages agonism by mediating constitutive endocytosis

scientific article published on 18 March 2003

The chemokine system -- a major regulator of angiogenesis in health and disease

scientific article

The frequency of cytomegalovirus non-ELR UL146 genotypes in neonates with congenital CMV disease is comparable to strains in the background population

scientific article published on 26 April 2021

The future of antiviral immunotoxins

scientific article published on 04 January 2016

The glucagon-like peptide 2 receptor is expressed in enteric neurons and not in the epithelium of the intestine

scientific article published on 06 March 2015

The impact of short-chain fatty acids on GLP-1 and PYY secretion from the isolated perfused rat colon

scientific article published on 01 March 2018

The minor binding pocket: a major player in 7TM receptor activation

scientific article published on 25 September 2010

The non-ELR CXC chemokine encoded by human cytomegalovirus UL146 genotype 5 contains a C-terminal β-hairpin and induces neutrophil migration as a selective CXCR2 agonist

scientific article published on 10 March 2022

Transfer of liraglutide from blood to cerebrospinal fluid is minimal in patients with type 2 diabetes

scientific article published on 31 July 2015

Transgenic rescue of adipocyte glucose-dependent insulinotropic polypeptide receptor expression restores high fat diet-induced body weight gain

scientific article published on 25 October 2011

Truncation of CXCL12 by CD26 reduces its CXC chemokine receptor 4- and atypical chemokine receptor 3-dependent activity on endothelial cells and lymphocytes

scientific article published on 16 March 2017

Tumorigenesis induced by the HHV8-encoded chemokine receptor requires ligand modulation of high constitutive activity.

scientific article

Varicella zoster virus glycoprotein C increases chemokine-mediated leukocyte migration.

scientific article

Vasopressin receptors V1a and V2 are not osmosensors

scientific article

Viral GPCR US28 can signal in response to chemokine agonists of nearly unlimited structural degeneracy.

scientific article published on 8 June 2018

Virally encoded chemokines and chemokine receptors in the role of viral infections

scientific article

Virus-encoded chemokine receptors--putative novel antiviral drug targets

scientific article