Muscarinic acetylcholine receptors: novel opportunities for drug development

Development of M1 mAChR Allosteric and Bitopic Ligands: Prospective Therapeutics for the Treatment of Cognitive Deficits

(2013) Briana J. Davie et al.   ACS Chemical Neuroscience

The Dynamic Process of β2-Adrenergic Receptor Activation

(2013) Rie Nygaard et al.   CELL

Inhibition of Leptin Regulation of Parasympathetic Signaling as a Cause of Extreme Body Weight-Associated Asthma

(2013) Emilio Arteaga-Solis et al.   Cell Metabolism

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease

(2013) Bruce J. Melancon et al.   DRUG DISCOVERY TODAY

Chronic activation of a designer Gq-coupled receptor improves β cell function

(2013) Shalini Jain et al.   JOURNAL OF CLINICAL INVESTIGATION

Molecular Basis for the Long Duration of Action and Kinetic Selectivity of Tiotropium for the Muscarinic M3 Receptor

(2013) Christofer S. Tautermann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Emerging paradigms in GPCR allostery: implications for drug discovery

(2013) Denise Wootten et al.   NATURE REVIEWS DRUG DISCOVERY

Structural Basis for Molecular Recognition at Serotonin Receptors

(2013) C. Wang et al.   SCIENCE

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Autonomic Nerve Development Contributes to Prostate Cancer Progression

(2013) C. Magnon et al.   SCIENCE

The worldwide diabetes epidemic

(2013) David W. Lam et al.   Current Opinion in Endocrinology Diabetes and Obesity

Heterotropic Cooperativity within and between Protomers of an Oligomeric M2 Muscarinic Receptor

(2012) Rabindra V. Shivnaraine et al.   BIOCHEMISTRY

Micro-crystallography comes of age

(2012) Janet L Smith et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

(2012) Kazuko Haga et al.   NATURE

Structure and dynamics of the M3 muscarinic acetylcholine receptor

(2012) Andrew C. Kruse et al.   NATURE

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

(2012) J. Robert Lane et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling

(2012) Andreas Bock et al.   Nature Communications

Muscarinic Acetylcholine Receptor Subtypes as Potential Drug Targets for the Treatment of Schizophrenia, Drug Abuse, and Parkinson’s Disease

(2011) Ditte Dencker et al.   ACS Chemical Neuroscience

Loss of Muscarinic M1 Receptor Exacerbates Alzheimer's Disease–Like Pathology and Cognitive Decline

(2011) Rodrigo Medeiros et al.   AMERICAN JOURNAL OF PATHOLOGY

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

(2011) Celine Valant et al.   Annual Review of Pharmacology and Toxicology

Muscarinic receptor subtype-3 gene ablation and scopolamine butylbromide treatment attenuate small intestinal neoplasia in Apcmin/+ mice

(2011) J.-P. Raufman et al.   CARCINOGENESIS

Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors

(2011) Wayne Stallaert et al.   Expert Opinion on Drug Discovery

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

(2011) Meritxell Canals et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Allosteric Modulation of Seven Transmembrane Spanning Receptors: Theory, Practice, and Opportunities for Central Nervous System Drug Discovery

(2011) Bruce J. Melancon et al.   JOURNAL OF MEDICINAL CHEMISTRY

Involvement of a Subpopulation of Neuronal M4 Muscarinic Acetylcholine Receptors in the Antipsychotic-like Effects of the M1/M4 Preferring Muscarinic Receptor Agonist Xanomeline

(2011) D. Dencker et al.   JOURNAL OF NEUROSCIENCE

Alzheimer's disease

(2011) Clive Ballard et al.   LANCET

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

(2011) Guillaume Lebon et al.   NATURE

Structure of the human histamine H1 receptor complex with doxepin

(2011) Tatsuro Shimamura et al.   NATURE

Crystal structure of metarhodopsin II

(2011) Hui-Woog Choe et al.   NATURE

The structural basis of agonist-induced activation in constitutively active rhodopsin

(2011) Jörg Standfuss et al.   NATURE

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Muscarinic and Nicotinic Acetylcholine Receptor Agonists and Allosteric Modulators for the Treatment of Schizophrenia

(2011) Carrie K Jones et al.   NEUROPSYCHOPHARMACOLOGY

Increased cocaine self-administration in M4 muscarinic acetylcholine receptor knockout mice

(2011) Lene S. Schmidt et al.   PSYCHOPHARMACOLOGY

Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice

(2011) Morgane Thomsen et al.   PSYCHOPHARMACOLOGY

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Allostery in GPCRs: ‘MWC’ revisited

(2011) Meritxell Canals et al.   TRENDS IN BIOCHEMICAL SCIENCES

Allosteric Receptors: From Electric Organ to Cognition

(2010) Jean-Pierre Changeux   Annual Review of Pharmacology and Toxicology

Rational design of dualsteric GPCR ligands: quests and promise

(2010) Klaus Mohr et al.   BRITISH JOURNAL OF PHARMACOLOGY

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

(2010) S Suratman et al.   BRITISH JOURNAL OF PHARMACOLOGY

Signaling through the M3 Muscarinic Receptor Favors Bone Mass Accrual by Decreasing Sympathetic Activity

(2010) Yu Shi et al.   Cell Metabolism

AGAP1/AP-3-dependent endocytic recycling of M5 muscarinic receptors promotes dopamine release

(2010) Jacob Bendor et al.   EMBO JOURNAL

Beneficial Metabolic Effects Caused by Persistent Activation of β-Cell M3Muscarinic Acetylcholine Receptors in Transgenic Mice

(2010) Dinesh Gautam et al.   ENDOCRINOLOGY

Identification of Orthosteric and Allosteric Site Mutations in M2Muscarinic Acetylcholine Receptors That Contribute to Ligand-selective Signaling Bias

(2010) Karen J. Gregory et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Gq/G11-mediated signaling pathway is critical for autocrine potentiation of insulin secretion in mice

(2010) Antonia Sassmann et al.   JOURNAL OF CLINICAL INVESTIGATION

Deletion of M1 Muscarinic Acetylcholine Receptors Increases Amyloid Pathology In Vitro and In Vivo

(2010) A. A. Davis et al.   JOURNAL OF NEUROSCIENCE

A Subpopulation of Neuronal M4 Muscarinic Acetylcholine Receptors Plays a Critical Role in Modulating Dopamine-Dependent Behaviors

(2010) J. Jeon et al.   JOURNAL OF NEUROSCIENCE

Orthosteric and Allosteric Modes of Interaction of Novel Selective Agonists of the M1 Muscarinic Acetylcholine Receptor

(2010) V. A. Avlani et al.   MOLECULAR PHARMACOLOGY

Maltose–neopentyl glycol (MNG) amphiphiles for solubilization, stabilization and crystallization of membrane proteins

(2010) Pil Seok Chae et al.   NATURE METHODS

Teaching old receptors new tricks: biasing seven-transmembrane receptors

(2010) Sudarshan Rajagopal et al.   NATURE REVIEWS DRUG DISCOVERY

Allosteric modulation of G protein-coupled receptors: A pharmacological perspective

(2010) Peter Keov et al.   NEUROPHARMACOLOGY

Presynaptic m1 muscarinic receptors are necessary for mGluR long-term depression in the hippocampus

(2010) A. Kamsler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1

(2010) K. C. Kong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The M3-muscarinic receptor regulates learning and memory in a receptor phosphorylation/arrestin-dependent manner

(2010) B. Poulin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

Cholinergic Functioning in Stimulant Addiction

(2009) Mehmet Sofuoglu et al.   CNS DRUGS

Hepatic Muscarinic Acetylcholine Receptors Are Not Critically Involved in Maintaining Glucose Homeostasis in Mice

(2009) Jian H. Li et al.   DIABETES

A Selective Allosteric Potentiator of the M1 Muscarinic Acetylcholine Receptor Increases Activity of Medial Prefrontal Cortical Neurons and Restores Impairments in Reversal Learning

(2009) J. K. Shirey et al.   JOURNAL OF NEUROSCIENCE

Attenuation of Cocaine's Reinforcing and Discriminative Stimulus Effects via Muscarinic M1 Acetylcholine Receptor Stimulation

(2009) M. Thomsen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators

(2009) Anna Kebig et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Schizophrenia

(2009) Jim van Os et al.   LANCET

Orthosteric/Allosteric Bitopic Ligands: Going Hybrid at GPCRs

(2009) C. Valant et al.   MOLECULAR INTERVENTIONS

Crystallizing membrane proteins using lipidic mesophases

(2009) Martin Caffrey et al.   Nature Protocols

Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation

(2009) L. Ma et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Neuronal M3 muscarinic acetylcholine receptors are essential for somatotroph proliferation and normal somatic growth

(2009) D. Gautam et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A chemical-genetic approach to study G protein regulation of β cell function in vivo

(2009) Jean-Marc Guettier et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

(2009) P. Jeffrey Conn et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Muscarinic receptors and ligands in cancer

(2008) Nirish Shah et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Selective Muscarinic Receptor Agonist Xanomeline as a Novel Treatment Approach for Schizophrenia

(2008) Anantha Shekhar et al.   AMERICAN JOURNAL OF PSYCHIATRY

Genetic Ablation of M3 Muscarinic Receptors Attenuates Murine Colon Epithelial Cell Proliferation and Neoplasia

(2008) J.-P. Raufman et al.   CANCER RESEARCH

Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity

(2008) Johannes Antony et al.   FASEB JOURNAL

A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity

(2008) Celine Valant et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Selective Allosteric Activator of the M1 Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats

(2008) C. K. Jones et al.   JOURNAL OF NEUROSCIENCE

Two-State Models and the Analysis of the Allosteric Effect of Gallamine at the M2 Muscarinic Receptor

(2008) F. J. Ehlert et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Binding of Orthosteric Ligands to the Allosteric Site of the M2 Muscarinic Cholinergic Receptor

(2008) D. S. Redka et al.   MOLECULAR PHARMACOLOGY

Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity

(2008) J. E. Marlo et al.   MOLECULAR PHARMACOLOGY

Structure of a β1-adrenergic G-protein-coupled receptor

(2008) Tony Warne et al.   NATURE

Crystal structure of opsin in its G-protein-interacting conformation

(2008) Patrick Scheerer et al.   NATURE

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia

(2008) W. Y. Chan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Muscarinic acetylcholine receptors as CNS drug targets

(2007) Christopher J. Langmead et al.   PHARMACOLOGY & THERAPEUTICS