M. Canals

发表

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

Albert C. Pan, R. Dror, D. Shaw, 2013, Nature.

Intramembrane receptor–receptor interactions: a novel principle in molecular medicine

K. Fuxe, D. Marcellino, A. Rivera, 2006, Journal of Neural Transmission.

Detection and Quantification of Allosteric Modulation of Endogenous M4 Muscarinic Acetylcholine Receptor Using Impedance-Based Label-Free Technology in a Neuronal Cell Line

P. Sexton, A. Christopoulos, M. Canals, 2015, Journal of biomolecular screening.

Adenosine A2A-dopamine D2 receptor-receptor heteromers. Targets for neuro-psychiatric disorders.

K. Fuxe, D. Marcellino, L. Agnati, 2004, Parkinsonism & related disorders.

Pharmacological modulation of chemokine receptor function

R. Leurs, C. de Graaf, H. Vischer, 2012, British journal of pharmacology.

Up-regulation of the Angiotensin II Type 1 Receptor by the MAS Proto-oncogene Is Due to Constitutive Activation of Gq/G11 by MAS*

G. Milligan, M. Canals, Laura Jenkins, 2006, Journal of Biological Chemistry.

OZITX, a pertussis toxin-like protein for occluding inhibitory G protein signalling including Gαz

J. R. Lane, Lei Shi, J. Javitch, 2022, Communications biology.

Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors

Davide Provasi, Arthur Christopoulos, Marta Filizola, 2016, ACS chemical biology.

Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor.

Kathryn E. Livingston, A. Christopoulos, M. Banks, 2015, Journal of medicinal chemistry.

Oligomeric structure of the α1b-adrenoceptor: Comparisons with rhodopsin

G. Milligan, J. Pediani, M. Canals, 2006, Vision Research.

Homodimerization of adenosine A2A receptors: qualitative and quantitative assessment by fluorescence and bioluminescence energy transfer

K. Fuxe, D. Marcellino, L. Agnati, 2003, Journal of neurochemistry.

Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

J. R. Lane, M. Kassiou, S. Schulz, 2020, Science Signaling.

Novel Dual-Target μ-Opioid Receptor and Dopamine D3 Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.

V. Katritch, A. Newman, Alessandro Bonifazi, 2021, Journal of medicinal chemistry.

A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptor

Andrew M. Piggott, R. Sessions, A-M Wang, 2019, Proceedings of the National Academy of Sciences.

Glutamate mGlu5-adenosine A2A-dopamine D2 receptor interactions in the striatum. Implications for drug therapy in neuro-psychiatric disorders and drug abuse

K. Fuxe, D. Marcellino, L. Agnati, 2003 .

GRK Mediates μ-Opioid Receptor Plasma Membrane Reorganization

S. Briddon, M. Canals, M. Halls, 2019, Front. Mol. Neurosci..

GRKs as Key Modulators of Opioid Receptor Function

J. R. Lane, M. Canals, Laura Lemel, 2020, Cells.

Endothelin-converting Enzyme 1 and β-Arrestins Exert Spatiotemporal Control of Substance P-induced Inflammatory Signals*

F. Cattaruzza, C. Pothoulakis, H. Koon, 2014, The Journal of Biological Chemistry.

Systematic Assessment of Chemokine Signaling at Chemokine Receptors CCR4, CCR7 and CCR10

J. R. Lane, M. Stone, M. Canals, 2021, International journal of molecular sciences.

Atypical opioid receptors: unconventional biology and therapeutic opportunities.

E. Kostenis, M. Canals, M. Meyrath, 2021, Pharmacology & therapeutics.

Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.

Leigh A. Stoddart, S. Briddon, P. Scammells, 2015, Journal of medicinal chemistry.

Themed Section: Opioids: New Pathways to Functional Selectivity

A. Christopoulos, M. Canals, G. Thompson, 2014 .

Protein Kinase D and Gβγ Subunits Mediate Agonist-evoked Translocation of Protease-activated Receptor-2 from the Golgi Apparatus to the Plasma Membrane*

S. Vanner, N. Bunnett, D. Poole, 2016, The Journal of Biological Chemistry.

Allosteric Modulation of M1 Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking*

P. Sexton, A. Christopoulos, N. Lambert, 2014, The Journal of Biological Chemistry.

Chemical subtleties in small-molecule modulation of peptide receptor function: the case of CXCR3 biaryl-type ligands.

I. D. de Esch, R. Leurs, C. de Graaf, 2012, Journal of medicinal chemistry.

Pharmacological characterization of a small‐molecule agonist for the chemokine receptor CXCR3

R. Leurs, H. Vischer, D. Verzijl, 2012, British journal of pharmacology.

1 G Protein-Coupled Receptors are Dynamic Regulators of Digestion and Targets for Digestive Diseases Short Title : GPCRs and Digestive Disease

N. Bunnett, N. Veldhuis, D. Poole, 2019 .

Influence of Chemokine N-Terminal Modification on Biased Agonism at the Chemokine Receptor CCR1

J. R. Lane, M. Stone, M. Canals, 2019, International journal of molecular sciences.

Evaluation and extension of the two-site, two-step model for binding and activation of the chemokine receptor CCR1

J. R. Lane, R. Payne, M. Stone, 2018, The Journal of Biological Chemistry.

Glycosylation Regulates N-Terminal Proteolysis and Activity of the Chemokine CCL14.

R. Payne, M. Stone, M. Larance, 2021, ACS chemical biology.

Cannabinoid receptor type 1 protects against age-related osteoporosis by regulating osteoblast and adipocyte differentiation in marrow stromal cells.

G. Milligan, S. Ralston, D. Baker, 2009, Cell metabolism.

Phosphoproteomic characterization of the signaling network resulting from activation of the chemokine receptor CCR2

Anup D. Shah, M. Stone, S. Foster, 2020, The Journal of Biological Chemistry.

Major: Biological Sciences Pharmacology Biased μ-opioid analgesics derived from a novel tetrapeptide class found in an Australian fungus

Andrew M. Piggott, R. Sessions, E. Lacey, 2019 .

Mu and Delta Opioid Receptors Are Coexpressed and Functionally Interact in the Enteric Nervous System of the Mouse Colon

A. Christopoulos, D. Massotte, R. A. Ceredig, 2019, Cellular and molecular gastroenterology and hepatology.

Abdul-Ridha, Alaa and Lane, J. Robert and Mistry, Shailesh N. and Lopez, Laura and Sexton, Patrick M. and Scammells, Peter J. and Christopoulos, Arthur and Canals, Meritxell (2014) Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine

Shailesh N Mistry, P. Sexton, A. Christopoulos, 2016 .

Critical Assessment of G Protein-Biased Agonism at the μ-Opioid Receptor.

S. Schulz, M. Canals, E. Kelly, 2020, Trends in pharmacological sciences.

Multisite phosphorylation is required for sustained interaction with GRKs and arrestins in mediating rapid mu-opioid receptor desensitization.

J. MacDonald, M. Bünemann, C. Krasel, 2019 .

Multisite phosphorylation is required for sustained interaction with GRKs and arrestins during rapid μ-opioid receptor desensitization

S. Schulz, M. Bünemann, C. Krasel, 2018, Science Signaling.

Agonist-biased Trafficking of Somatostatin Receptor 2A in Enteric Neurons*

N. Bunnett, D. Poole, M. Canals, 2013, The Journal of Biological Chemistry.

Distribution and trafficking of the μ-opioid receptor in enteric neurons of the guinea pig.

N. Bunnett, D. Poole, M. Canals, 2016, American journal of physiology. Gastrointestinal and liver physiology.

The role of kinetic context in apparent biased agonism at GPCRs

Arthur Christopoulos, Patrick M Sexton, Jonathan A Javitch, 2016, Nature Communications.

Adenosine A 2 A Receptor and Dopamine D 3 Receptor Interactions : Evidence of Functional A 2 A / D 3 Heteromeric Complexes

K. Fuxe, D. Marcellino, L. Agnati, 2005 .

Biological redundancy of endogenous GPCR ligands in the gut and the potential for endogenous functional selectivity

D. Poole, M. Canals, Georgina L. Thompson, 2014, Front. Pharmacol..

Clathrin and GRK2/3 inhibitors block delta opioid receptor internalization in myenteric neurons and inhibit neuromuscular transmission in the mouse colon.

N. Veldhuis, D. Poole, M. Canals, 2019, American journal of physiology. Gastrointestinal and liver physiology.

Tyrosine Sulfation of Chemokine Receptor CCR2 Enhances Interactions with Both Monomeric and Dimeric Forms of the Chemokine Monocyte Chemoattractant Protein-1 (MCP-1)*

A. Christopoulos, M. Hickey, R. Payne, 2013, The Journal of Biological Chemistry.

Structure-Based Ligand Discovery Targeting Orthosteric and Allosteric Pockets of Dopamine Receptors

Ruben Abagyan, Vadim Cherezov, Vsevolod Katritch, 2013, Molecular Pharmacology.

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies.

S. Briddon, P. Scammells, M. Canals, 2018, Journal of medicinal chemistry.

The α1b-Adrenoceptor Exists as a Higher-Order Oligomer: Effective Oligomerization Is Required for Receptor Maturation, Surface Delivery, and Function

Graeme Milligan, Meritxell Canals, G. Milligan, 2007, Molecular Pharmacology.

Experimental considerations for the assessment of in vivo and in vitro opioid pharmacology.

M. Canals, Rob Hill, R. Hill, 2021, Pharmacology & therapeutics.

Constitutive Activity of the Cannabinoid CB1 Receptor Regulates the Function of Co-expressed Mu Opioid Receptors*

Graeme Milligan, Meritxell Canals, G. Milligan, 2008, Journal of Biological Chemistry.

Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief

Pierangelo Geppetti, Martin J. Scanlon, Christopher J. H. Porter, 2017, Science Translational Medicine.

Coaggregation, Cointernalization, and Codesensitization of Adenosine A2A Receptors and Dopamine D2Receptors*

Michele Zoli, Luigi F Agnati, Meritxell Canals, 2002, The Journal of Biological Chemistry.

Anxiety enhances pain in a model of osteoarthritis and is associated with altered endogenous opioid function and reduced opioid analgesia

D. Walsh, J. Burston, S. Woodhams, 2020, bioRxiv.

Structural basis of receptor sulfotyrosine recognition by a CC chemokine: the N-terminal region of CCR3 bound to CCL11/eotaxin-1.

Arthur Christopoulos, Meritxell Canals, A. Christopoulos, 2014, Structure.

Plasma membrane localization of the μ-opioid receptor controls spatiotemporal signaling

Meritxell Canals, Nigel W. Bunnett, Daniel P. Poole, 2016, Science Signaling.

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2

Benjamin T. Porebski, J. R. Lane, M. Stone, 2017, Science Signaling.

Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists.

I. D. de Esch, R. Leurs, C. de Graaf, 2012, European journal of medicinal chemistry.

Working memory deficits in transgenic rats overexpressing human adenosine A2A receptors in the brain

Michael Bader, Francisco Ciruela, Meritxell Canals, 2007, Neurobiology of Learning and Memory.

G-Protein-Coupled Receptors Are Dynamic Regulators of Digestion and Targets for Digestive Diseases.

B. Schmidt, N. Bunnett, N. Veldhuis, 2019, Gastroenterology.

Inflammation-associated changes in DOR expression and function in the mouse colon.

J. Fichna, N. Bunnett, C. Nowell, 2018, American journal of physiology. Gastrointestinal and liver physiology.

Regulation of heptaspanning-membrane-receptor function by dimerization and clustering.

Francisco Ciruela, Meritxell Canals, Daniel Marcellino, 2003, Trends in biochemical sciences.

Ligand-dependent spatiotemporal signaling profiles of the μ-opioid receptor are controlled by distinct protein-interaction networks

M. Canals, R. Schittenhelm, Cheng Huang, 2019, The Journal of Biological Chemistry.

Molecular mechanisms involved in the adenosine A1 and A2A receptor‐induced neuronal differentiation in neuroblastoma cells and striatal primary cultures

K. Fuxe, W. Staines, L. Agnati, 2005, Journal of neurochemistry.

Presynaptic Control of Striatal Glutamatergic Neurotransmission by Adenosine A1–A2A Receptor Heteromers

Graeme Milligan, Francisco Ciruela, Meritxell Canals, 2006, The Journal of Neuroscience.

Adenosine A2A Receptor and Dopamine D3 Receptor Interactions: Evidence of Functional A2A/D3 Heteromeric Complexes

K. Fuxe, D. Marcellino, L. Agnati, 2005, Molecular Pharmacology.

Adenosine A2A-Dopamine D2 Receptor-Receptor Heteromerization

Francesca Fanelli, Michel Bouvier, Luigi F Agnati, 2003, Journal of Biological Chemistry.

The Bile Acid Receptor TGR5 Does Not Interact with β-Arrestins or Traffic to Endosomes but Transmits Sustained Signals from Plasma Membrane Rafts*

N. Lambert, F. Alemi, G. Cottrell, 2013, The Journal of Biological Chemistry.

Adenosine A2A and dopamine D2 heteromeric receptor complexes and their function

Luigi F. Agnati, Meritxell Canals, Daniel Marcellino, 2007, Journal of Molecular Neuroscience.

Ticks from diverse genera encode chemokine-inhibitory evasin proteins

R. Payne, M. Stone, M. Rodriguez Valle, 2017, The Journal of Biological Chemistry.

Cell surface delivery and structural re-organization by pharmacological chaperones of an oligomerization-defective α1b-adrenoceptor mutant demonstrates membrane targeting of GPCR oligomers

G. Milligan, M. Canals, J. López-Giménez, 2008, The Biochemical journal.

Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations

S. Charlton, O. Kleifeld, B. A. Evans, 2018, Science Signaling.

COMMENTARY—THE MANY FACETS OF OPIOID RECEPTOR PHOSPHORYLATION The Complex Roles of m-Opioid Receptor Phosphorylation: A Key Determinant in Receptor Signaling and Regulation

M. Canals, 2015 .

Orexin-1 Receptor-Cannabinoid CB1 Receptor Heterodimerization Results in Both Ligand-dependent and -independent Coordinated Alterations of Receptor Localization and Function*

G. Milligan, J. Pediani, S. Milasta, 2006, Journal of Biological Chemistry.

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

P. Sexton, A. Christopoulos, M. Canals, 2016, Biochemical pharmacology.

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

P. Sexton, A. Christopoulos, M. Canals, 2015, Molecular Pharmacology.

Novel GPCR paradigms at the μ‐opioid receptor

A. Christopoulos, M. Canals, E. Kelly, 2015, British journal of pharmacology.

Agonist activation of the G protein‐coupled receptor GPR35 involves transmembrane domain III and is transduced via Gα13 and β‐arrestin‐2

G. Milligan, E. Alvarez-Curto, M. Canals, 2011, British journal of pharmacology.

Protease-activated receptor-2 in endosomes signals persistent pain of irritable bowel syndrome

Brian L. Schmidt, Rocco Latorre, Christopher J. H. Porter, 2018, Proceedings of the National Academy of Sciences.

The Life Cycle of the Mu-Opioid Receptor.

M. Canals, L. Hipólito, Javier Cuitavi, 2020, Trends in biochemical sciences.

Combining mass spectrometry and pull-down techniques for the study of receptor heteromerization. Direct epitope-epitope electrostatic interactions between adenosine A2A and dopamine D2 receptors.

K. Fuxe, D. Marcellino, L. Agnati, 2004, Analytical chemistry.

Regulation of G protein-coupled receptors by allosteric ligands.

J. R. Lane, M. Canals, J. R. Lane, 2013, ACS chemical neuroscience.

Receptor heteromerization in adenosine A2A receptor signaling

L F Agnati, K Fuxe, K. Jacobsen, 2003, Neurology.

OZITX, a pertussis toxin-like protein for occluding inhibitory G protein signalling including Gαz

J. R. Lane, Lei Shi, J. Javitch, 2022, Communications Biology.

Opioid Pharmacology under the Microscope

M. von Zastrow, D. Jullié, M. Canals, 2020, Molecular Pharmacology.

Agonist-dependent development of delta opioid receptor tolerance in the colon

N. Veldhuis, D. Poole, M. Canals, 2019, Cellular and Molecular Life Sciences.

Agonist-dependent development of delta opioid receptor tolerance in the colon

N. Veldhuis, D. Poole, M. Canals, 2019, Cellular and Molecular Life Sciences.

Allostery in GPCRs: 'MWC' revisited.

P. Sexton, A. Christopoulos, M. Canals, 2011, Trends in biochemical sciences.

The respiratory depressant effects of mitragynine are limited by its conversion to 7‐OH mitragynine

J. R. Lane, J. Javitch, M. Canals, 2022, British journal of pharmacology.

Identification of Overlapping but Differential Binding Sites for the High-Affinity CXCR3 Antagonists NBI-74330 and VUF11211

I. D. de Esch, R. Leurs, C. de Graaf, 2014, Molecular Pharmacology.

Design and Receptor Interactions of Obligate Dimeric Mutant of Chemokine Monocyte Chemoattractant Protein-1 (MCP-1)*

A. Christopoulos, R. Payne, M. Stone, 2012, The Journal of Biological Chemistry.

Ubiquitination of CXCR7 Controls Receptor Trafficking

R. Leurs, M. Smit, M. Canals, 2012, PloS one.

Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission

Pierangelo Geppetti, Christopher J. H. Porter, Zhijian Cai, 2017, Proceedings of the National Academy of Sciences.

Molecular Determinants of Allosteric Modulation at the M1 Muscarinic Acetylcholine Receptor*

Arthur Christopoulos, Patrick M Sexton, Laura López, 2014, The Journal of Biological Chemistry.

Endosomal signaling of delta opioid receptors is an endogenous mechanism and therapeutic target for relief from inflammatory pain

B. Schmidt, K. Leong, S. Vanner, 2020, Proceedings of the National Academy of Sciences.

New phosphosite-specific antibodies to unravel the role of GRK phosphorylation in dopamine D2 receptor regulation and signaling

J. Javitch, S. Schulz, M. Canals, 2021, Scientific Reports.

Sequential Conformational Rearrangements Dictate the Dynamics of Class C GPCR Activation

M. Canals, J. R. Lane, Meritxell Canals, 2012, Science Signaling.

Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors

Kathryn E. Livingston, J. Traynor, M. Stanczyk, 2018, Molecular Pharmacology.

Genetically Encoded FRET Biosensors to Illuminate Compartmentalised GPCR Signalling.

Meritxell Canals, M. Canals, Michelle L Halls, 2017, Trends in pharmacological sciences.

Allosteric Modulation of a Chemogenetically Modified G Protein-Coupled Receptor

P. Sexton, A. Christopoulos, M. Canals, 2013, Molecular Pharmacology.

Detection and Quantification of Intracellular Signaling Using FRET-Based Biosensors and High Content Imaging.

C. Nowell, D. Poole, M. Canals, 2015, Methods in molecular biology.

A Monod-Wyman-Changeux Mechanism Can Explain G Protein-coupled Receptor (GPCR) Allosteric Modulation*

P. Sexton, A. Christopoulos, P. Scammells, 2011, The Journal of Biological Chemistry.

Opioid-Induced Pronociceptive Signaling in the Gastrointestinal Tract Is Mediated by Delta-Opioid Receptor Signaling

S. Vanner, N. Bunnett, C. López-López, 2022, The Journal of Neuroscience.

Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor*

Arthur Christopoulos, Laura López, Patrick M. Sexton, 2014, The Journal of Biological Chemistry.

The role of GPCR dimerisation/oligomerisation in receptor signalling.

G. Milligan, J. Pediani, M. Canals, 2006, Ernst Schering Foundation symposium proceedings.

Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer

J. Arribas, M. Guzmán, G. Moreno-Bueno, 2019, Proceedings of the National Academy of Sciences.

Therapeutic targeting of HER 2-CB 2 R heteromers in HER 2-positive breast cancer

J. Arribas, G. Moreno-Bueno, V. Casadó, 2019 .

A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes

S. Hill, S. Briddon, T. P. Davis, 2021, The Journal of biological chemistry.

Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D3 (D3R) and μ-Opioid (MOR) Receptor Ligands as Potentially Safer Analgesics.

Antonina L. Nazarova, V. Katritch, J. R. Lane, 2023, Journal of medicinal chemistry.

Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1).

A. Christopoulos, M. Hickey, R. Payne, 2014, The Journal of Biological Chemistry.

The Complex Roles of μ-Opioid Receptor Phosphorylation: A Key Determinant in Receptor Signaling and Regulation

M. Canals, 2015, Molecular Pharmacology.

Proteomic Identification of Interferon-Induced Proteins with Tetratricopeptide Repeats as Markers of M1 Macrophage Polarization.

M. Stone, N. Borg, Antony Vinh, 2018, Journal of proteome research.

Running Title : Evidence for a conserved opioid receptor allosteric site Corresponding

Kathryn E. Livingston, J. Traynor, M. Stanczyk, 2017 .

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

Shailesh N Mistry, P. Sexton, A. Christopoulos, 2017 .

Acetylcholine Receptor Muscarinic 1 Modulation at the M Molecular Determinants of Allosteric Signal Transduction

Shailesh N Mistry, P. Sexton, A. Christopoulos, 2016 .

Muscarinic Acetylcholine Receptor 1 Structure-Function Relationships at the M Mechanistic Insights into Allosteric

P. Sexton, A. Christopoulos, P. Scammells, 2014 .