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List of works by Patrick M. Sexton

"Ins and outs" of seven-transmembrane receptor signalling to ERK.

scientific article

2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.

scientific article

3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists

scientific article

4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.

scientific article published in December 2015

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

scientific article published on 28 December 2018

A Hydrogen-Bonded Polar Network in the Core of the Glucagon-Like Peptide-1 Receptor Is a Fulcrum for Biased Agonism: Lessons from Class B Crystal Structures

scientific article

A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation

scientific article published on 15 November 2011

A kinetic view of GPCR allostery and biased agonism

scientific article published in August 2017

A new mechanism of allostery in a G protein-coupled receptor dimer

scientific article (publication date: September 2014)

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

scientific article

A nuclear transport inhibitor that modulates the unfolded protein response and provides in vivo protection against lethal dengue virus infection.

scientific article

A simple method to generate stable cell lines for the analysis of transient protein-protein interactions.

scientific article published on April 2013

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

scientific article published on 06 September 2016

Activation and allosteric modulation of a muscarinic acetylcholine receptor

scientific article

Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family Peptide receptor 3.

scientific article published on April 2009

Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology.

scientific article published on 13 July 2007

Allosteric Modulation of G Protein–Coupled Receptors

scientific article published on 01 January 2007

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening.

scientific article

Allosteric modulation of G protein-coupled receptors.

scientific article

Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.

scientific article published on 15 July 2010

Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking

scientific article

Allosteric modulation of a chemogenetically modified G protein-coupled receptor.

scientific article published on 29 November 2012

Allosteric modulation of endogenous metabolites as an avenue for drug discovery.

scientific article published on 10 May 2012

Allosteric modulation of muscarinic acetylcholine receptors

scientific article published in September 2007

Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes.

scientific article

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

scientific article published on 4 April 2016

Allostery in GPCRs: 'MWC' revisited.

scientific article published on 14 September 2011

Amylin is an agonist of the renal porcine calcitonin receptor

scientific article published on May 1994

An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology

scientific article published on 17 May 2016

Angiotensin II receptors in the kidney. Localization and physiological significance

scientific article published on 01 March 1990

Application of a kinetic model to the apparently complex behavior of negative and positive allosteric modulators of muscarinic acetylcholine receptors

scientific article

Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors

scientific article published on 24 April 2018

Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor

scientific article published on 20 June 2008

Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor

scientific article published on 4 June 2015

Biased Agonism of Endogenous Opioid Peptides at the μ-Opioid Receptor.

scientific article published on 26 May 2015

Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs

scientific article published on 20 February 2020

Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics

scientific article

Biologically active salmon calcitonin-like peptide is present in rat brain

scientific article published in November 1992

Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.

scientific article published on 25 April 2018

Bridging the gap: bitopic ligands of G-protein-coupled receptors.

scientific article

Calcitonin receptor antibodies in the identification of osteoclasts

scientific article published on 01 July 1999

Calcium inflow in cells transfected with cloned rat and porcine calcitonin receptors.

scientific article published on March 1995

Central nervous system binding sites for calcitonin and calcitonin gene-related peptide ⬇️

scientific article published on January 1, 1991

Characterization of amylin and calcitonin receptor binding in the mouse alpha-thyroid-stimulating hormone thyrotroph cell line

scientific article published on August 1997

Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2.

scientific article published on June 2005

Characterization of signal bias at the GLP-1 receptor induced by backbone modification of GLP-1.

scientific article published on 28 March 2017

Characterization of signalling and regulation of common calcitonin receptor splice variants and polymorphisms

scientific article

Coding GPCR-G protein specificity.

scientific article published on 11 July 2017

Coexpressed Class B G Protein-Coupled Secretin and GLP-1 Receptors Self- and Cross-Associate: Impact on Pancreatic Islets

scientific article published on 29 March 2017

Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research.

scientific article published on 10 May 2018

Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs

scientific article

Consequences of splice variation on Secretin family G protein-coupled receptor function

scientific article

Constitutive formation of oligomeric complexes between family B G protein-coupled vasoactive intestinal polypeptide and secretin receptors

scientific article published on 21 October 2005

Correspondence: Reply to 'Compound 17b and formyl peptide receptor biased agonism in relation to cardioprotective effects in ischaemia-reperfusion injury'.

scientific article published on 7 February 2018

Critical Role for the Second Extracellular Loop in the Binding of Both Orthosteric and Allosteric G Protein-coupled Receptor Ligands

scientific article published in Journal of Biological Chemistry

Cryo-EM structure of the active, G-protein complexed, human CGRP receptor

scientific article published in Nature

Cryo-electron microscopy structure of the glucagon receptor with a dual-agonist peptide

scientific article published on 05 May 2020

Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs

scientific article published on 23 July 2019

Crystal structure of the M5 muscarinic acetylcholine receptor

scientific article published on 26 November 2019

Delineating the mode of action of adenosine A1 receptor allosteric modulators

scientific article published on 14 June 2010

Detection and quantification of allosteric modulation of endogenous m4 muscarinic acetylcholine receptor using impedance-based label-free technology in a neuronal cell line.

scientific article published on 22 December 2014

Detection of novel functional selectivity at M3 muscarinic acetylcholine receptors using a Saccharomyces cerevisiae platform

scientific article published on April 2010

Determinants of 1-piperidinecarboxamide, N-[2-[[5-amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) affinity for calcitonin gene-r

scientific article published on 29 August 2006

Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding

scientific article

Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor

scientific article published on 9 September 2014

Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands

scientific article published on 24 January 2013

Differential engagement of polar networks in the glucagon-like peptide 1 receptor by endogenous variants of the glucagon-like peptide 1

scientific article published on 25 August 2018

Differential impact of amino acid substitutions on critical residues of the human glucagon-like peptide-1 receptor involved in peptide activity and small-molecule allostery.

scientific article published on 28 January 2015

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

scientific article published on 26 April 2018

Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs

scientific article

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity.

scientific article published in May 2018

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H receptor antagonists

article

Effects of conformational restriction of 2-amino-3-benzoylthiophenes on A(1) adenosine receptor modulation

scientific article published on September 2010

Electrophoretic mobility and glycosylation characteristics of heterogeneously expressed calcitonin receptors

scientific article published on February 1997

Emerging paradigms in GPCR allostery: implications for drug discovery ⬇️

scientific article published on August 1, 2013

Endogenous allosteric modulators of G protein-coupled receptors

scientific article

Engendering biased signalling from the calcium-sensing receptor for the pharmacotherapy of diverse disorders

scientific article published on March 2014

Evidence for a new subclass of calcitonin/ calcitonin gene-related peptide binding site in rat brain.

scientific article published on January 1988

Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy.

scientific article published on 28 September 2016

Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy.

scientific article published on 15 February 2018

Fluorescence resonance energy transfer analysis of secretin docking to its receptor: mapping distances between residues distributed throughout the ligand pharmacophore and distinct receptor residues

scientific article published on 7 September 2007

Function of the rat calcitonin receptors, C1a and C1b, expressed in Xenopus oocytes

scientific article published in January 1998

Functional Selectivity and Classical Concepts of Quantitative Pharmacology

scientific article

Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor

scientific article published on 8 May 2009

G Protein-Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus.

scientific article published in January 2018

G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor

scientific article

GPCR modulation by RAMPs

scientific article published in January 2006

GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1-2 September 2014.

scientific article published on 14 March 2015

Genetically encoded photocross-linkers determine the biological binding site of exendin-4 peptide in the N-terminal domain of the intact human glucagon-like peptide-1 receptor (GLP-1R)

scientific article

Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes ⬇️

scientific article

Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery.

scientific article

Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists

scientific article published on 07 September 2018

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).

scientific article

Hematological defects in the oc/oc mouse, a model of infantile malignant osteopetrosis

scientific article published on 01 September 2004

High throughput, quantitative analysis of human osteoclast differentiation and activity

scientific article published on 14 December 2016

Homologous regulation of the rat C1a calcitonin receptor (CTR) in nonosteoclastic cells is independent of CTR messenger ribonucleic acid changes and cyclic adenosine 3',5'-monophosphate-dependent protein kinase activation

scientific article published on November 1996

Homology modeling of GPCRs.

scientific article published in January 2009

Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function

scientific article published in October 2008

Identification of molecular phenotypes and biased signaling induced by naturally occurring mutations of the human calcium-sensing receptor.

scientific article

Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

scientific article published on 31 January 2013

Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor.

scientific article

Improving virtual screening of G protein-coupled receptors via ligand-directed modeling.

scientific article published on 13 November 2017

In vitro autoradiographic localization of amylin binding sites in rat brain

scientific article published on 01 September 1994

In vitro autoradiographic localization of calcitonin and amylin binding sites in monkey brain

scientific article

In vitro autoradiographic localization of the calcitonin receptor isoforms, C1a and C1b, in rat brain

scientific article published on 01 December 1995

Insights into interactions between the alpha-helical region of the salmon calcitonin antagonists and the human calcitonin receptor using photoaffinity labeling

scientific article published in June 2005

Interaction studies of multiple binding sites on m4 muscarinic acetylcholine receptors

scientific article published on 18 May 2006

International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands.

scientific article

International Union of Pharmacology. XXXII. The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors

scientific article (publication date: June 2002)

Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41.

scientific article

Isoform-Specific Biased Agonism of Histamine H3 Receptor Agonists

scientific article published on 18 November 2016

Isoforms of the rat calcitonin receptor: consequences for ligand binding and signal transduction

scientific article published on 01 July 1994

Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor

scientific article

Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists

scientific article published on 4 August 2015

Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy

scientific article published on 6 October 2016

Lipopolysaccharide supports survival and fusion of preosteoclasts independent of TNF-alpha, IL-1, and RANKL.

scientific article published in January 2002

Localization of binding sites for calcitonin gene-related peptide in rat brain by in vitro autoradiography

scientific article published in December 1986

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss

scientific article

Mechanisms of ERK1/2 regulation by seven-transmembrane-domain receptors.

scientific article

Mechanisms of signalling and biased agonism in G protein-coupled receptors

scientific article published on 01 October 2018

Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.

scientific article

Mini ReviewCalcitonin

article

Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery

scientific article published on 17 July 2013

Modulating receptor function through RAMPs: can they represent drug targets in themselves?

scientific article published on 16 January 2009

Molecular Basis for Binding and Subtype Selectivity of 1,4-Benzodiazepine Antagonist Ligands of the Cholecystokinin Receptor ⬇️

scientific article published on March 30, 2012

Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor

scientific article published on 27 December 2018

Molecular Basis of Secretin Docking to Its Intact Receptor Using Multiple Photolabile Probes Distributed throughout the Pharmacophore ⬇️

scientific article published on May 12, 2011

Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.

scientific article published on 10 December 2015

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators

scientific article published on 26 July 2016

Molecular approximations between residues 21 and 23 of secretin and its receptor: development of a model for peptide docking with the amino terminus of the secretin receptor

scientific article published on 2 May 2007

Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor.

scientific article published on 10 June 2013

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor.

scientific article published on 17 January 2014

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties

scientific article

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor

scientific article

Molecular pharmacology of class II G protein-coupled receptors. Introduction

scientific article published on 01 January 2002

Molecular pharmacology of the calcitonin receptor

scientific article (publication date: 2002)

Monotreme glucagon-like peptide-1 in venom and gut: one gene - two very different functions

scientific article published on 29 November 2016

Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function

scientific journal article

Multiple ramp domains are required for generation of amylin receptor phenotype from the calcitonin receptor gene product

scientific article published on 01 January 2000

Murine GPRC6A Mediates Cellular Responses to L-Amino Acids, but Not Osteocalcin Variants

scientific article published on 19 January 2016

Muscarinic M5 receptors modulate ethanol seeking in rats

scientific article published on 5 February 2018

Muscarinic acetylcholine receptors: novel opportunities for drug development

scientific article

New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug).

scientific article published on 15 July 2008

Novel Allosteric Modulators of G Protein-coupled Receptors

scientific article

Novel Irreversible Agonists Acting at the A1 Adenosine Receptor

scientific article

Novel receptor partners and function of receptor activity-modifying proteins

scientific article (publication date: 31 January 2003)

O-GlcNAc Engineering of GPCR Peptide-Agonists Improves Their Stability and in Vivo Activity

scientific article published on 16 August 2019

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor

scientific article published on 22 April 2010

Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.

scientific article published on June 2009

Overview of Receptor Allosterism

scientific article published on 01 December 2010

Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes

scientific article published on 3 February 2005

Pharmacology of 5HT(2C) receptor-mediated ERK1/2 phosphorylation: agonist-specific activation pathways and the impact of RNA editing

scientific article published on 31 August 2008

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex

scientific article published on 21 February 2018

Photoaffinity scanning in the mapping of the peptide receptor interface of class II G protein-coupled receptors.

scientific article published on April 2004

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations ⬇️

scientific article published on March 11, 2013

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.

scientific article

Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior

scientific article published on 14 September 2016

Positive allosteric mechanisms of adenosine A<sub>1</sub> receptor-mediated analgesia

scientific article published on 08 September 2021

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.

scientific article

Prediction of Loops in G Protein-Coupled Receptor Homology Models: Effect of Imprecise Surroundings and Constraints

scientific article published on 15 March 2016

Prediction of functionally selective allosteric interactions at an M3 muscarinic acetylcholine receptor mutant using Saccharomyces cerevisiae

scientific article published on 13 May 2010

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects

scientific article published on 11 October 2011

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

scientific article

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor

scientific article published on 17 May 2018

Procalcitonin has bioactivity at calcitonin receptor family complexes: potential mediator implications in sepsis

scientific article

Prolonged calcitonin receptor signaling by salmon, but not human calcitonin, reveals ligand bias

scientific article

Purification of calcitonin-like peptides from rat brain and pituitary

scientific article

Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery

scientific article published on 12 November 2015

RAMPs as Drug Targets ⬇️

scientific article published on January 1, 2012

Recent advances in the determination of G protein-coupled receptor structures.

scientific article published on 13 March 2018

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function.

scientific article published on February 2013

Receptor activity modifying proteins and their potential as drug targets

scientific article published on January 2010

Receptor activity modifying proteins.

scientific article

Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors

scientific article published on 3 July 2008

Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators

scientific article

Regulation of serotonin 5-HT2C receptors by chronic ligand exposure.

scientific article

Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry

scientific article

Restoring Agonist Function at a Chemogenetically Modified M1 Muscarinic Acetylcholine Receptor

scientific article published on 16 November 2020

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

scientific article

Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

scientific article published on 28 September 2016

Routine sub-2.5 Å cryo-EM structure determination of GPCRs

scientific article published on 15 July 2021

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function.

scientific article published on 6 December 2011

Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation

scientific article published on 6 December 2011

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

scientific article published on 11 March 2014

Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin.

scientific article published on 28 August 2012

Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice.

scientific article published on 07 February 2017

Spatial proximity between a photolabile residue in position 19 of salmon calcitonin and the amino terminus of the human calcitonin receptor

scientific article published on 17 November 2003

Stimulus bias provides evidence for conformational constraints in the structure of a G protein-coupled receptor

scientific article

Structural and functional insights into the juxtamembranous amino-terminal tail and extracellular loop regions of class B GPCRs.

scientific article published on March 2014

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

scientific article published on 13 October 2013

Structural basis of Gs and Gi recognition by the human glucagon receptor

scientific article

Structural biology: meet the B family

scientific article published on 17 July 2013

Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.

scientific article

Structural features embedded in G protein-coupled receptor co-crystal structures are key to their success in virtual screening

scientific article

Structural insights into G-protein-coupled receptor allostery

scientific article published in Nature

Structure and dynamics of the active Gs-coupled human secretin receptor

scientific article published on 18 August 2020

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity

scientific article published in February 2017

Structure of the adenosine-bound human adenosine A1 receptor–Gi complex

scientific article published in Nature

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor

scientific article published on 16 February 2018

Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors

scientific article published on 24 May 2007

Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity

scientific article published on 04 June 2021

Structure–Function Studies of Muscarinic Acetylcholine Receptors ⬇️

scientific article published on January 1, 2012

Structure–function analysis of amino acid 74 of human RAMP1 and RAMP3 and its role in peptide interactions with adrenomedullin and calcitonin gene-related peptide receptors

scientific article published in May 2011

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.

scientific article published on 17 February 2012

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004.

scientific article published on 17 April 2015

Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.

scientific article published on 5 June 2014

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

scientific article published on 17 June 2013

Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor.

scientific article

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

scientific article

The complexity of signalling mediated by the glucagon-like peptide-1 receptor.

scientific article published on April 2016

The effect of social isolation on rat brain expression of genes associated with endocannabinoid signaling.

scientific article published on 27 April 2010

The effects of C-terminal truncation of receptor activity modifying proteins on the induction of amylin receptor phenotype from human CTb receptors

scientific article published on 16 August 2007

The impact of orthosteric radioligand depletion on the quantification of allosteric modulator interactions

scientific article published on 5 March 2008

The ontogeny of [125I]rat-alpha-CGRP binding sites in the spinal cord of sheep: a prenatal and postnatal study

scientific article published on 01 September 1994

The receptor activity modifying protein family of G protein coupled receptor accessory proteins

scientific article published on June 2004

The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism.

scientific article

The role of kinetic context in apparent biased agonism at GPCRs

scientific article published on 24 February 2016

The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor.

scientific article published on 7 February 2011

The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor.

scientific article published on 4 May 2011

To Bind or Not to Bind: Unravelling GPCR Polypharmacology.

scientific article published in February 2018

Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors

scientific article published on 06 September 2018

Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor

scientific article published on 22 March 2016

Towards tissue-specific pharmacology: insights from the calcium-sensing receptor as a paradigm for GPCR (patho)physiological bias

scientific article published on 09 March 2015

Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism.

scientific article published in May 2018

Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 22 April 2020

Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 23 April 2020

Use of Backbone Modification To Enlarge the Spatiotemporal Diversity of Parathyroid Hormone Receptor-1 Signaling via Biased Agonism

scientific article published on 09 September 2019

Use of Cysteine Trapping to Map Spatial Approximations between Residues Contributing to the Helix N-capping Motif of Secretin and Distinct Residues within Each of the Extracellular Loops of Its Receptor

scientific article published on 6 January 2016

Utility of an "allosteric site-impaired" M2 muscarinic acetylcholine receptor as a novel construct for validating mechanisms of action of synthetic and putative endogenous allosteric modulators

scientific article published on 13 September 2018

Vascular and molecular pharmacology of the metabolically stable CGRP analogue, SAX

scientific article published on 10 April 2018

β-Arrestin-Biased Agonists of the GLP-1 Receptor from β-Amino Acid Residue Incorporation into GLP-1 Analogues.

scientific article published on 4 November 2016

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