Mechanistic Insights into Allosteric Structure-Function Relationships at the M1Muscarinic Acetylcholine Receptor

Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M1 positive allosteric modulators

(2014) Scott D. Kuduk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Muscarinic acetylcholine receptor X-ray structures: potential implications for drug development

(2014) Andrew C Kruse et al.   CURRENT OPINION IN PHARMACOLOGY

Molecular Mechanisms of Bitopic Ligand Engagement with the M1Muscarinic Acetylcholine Receptor

(2014) Peter Keov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular Determinants of Allosteric Modulation at the M1Muscarinic Acetylcholine Receptor

(2014) Alaa Abdul-Ridha et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

(2014) Nellie E Byun et al.   NEUROPSYCHOPHARMACOLOGY

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

A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor

(2013) Jeremy Shonberg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Pharmacological Profiling of Analogues of Benzyl Quinolone Carboxylic Acid (BQCA) as Allosteric Modulators of the M1 Muscarinic Receptor

(2013) Shailesh N. Mistry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

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

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

Development of allosteric modulators of GPCRs for treatment of CNS disorders

(2013) Hilary Highfield Nickols et al.   NEUROBIOLOGY OF DISEASE

Targeting Selective Activation of M1 for the Treatment of Alzheimer’s Disease: Further Chemical Optimization and Pharmacological Characterization of the M1 Positive Allosteric Modulator ML169

(2012) James C. Tarr et al.   ACS Chemical Neuroscience

Structure-Function of the G Protein–Coupled Receptor Superfamily

(2012) Vsevolod Katritch et al.   Annual Review of Pharmacology and Toxicology

Novel M1allosteric ligands: a patent review

(2012) Scott D Kuduk et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

The potent M1 receptor allosteric agonist GSK1034702 improves episodic memory in humans in the nicotine abstinence model of cognitive dysfunction

(2012) Pradeep J. Nathan et al.   INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY

Conopeptide ρ-TIA Defines a New Allosteric Site on the Extracellular Surface of the α1B-Adrenoceptor

(2012) Lotten Ragnarsson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

The GPCR Network: a large-scale collaboration to determine human GPCR structure and function

(2012) Raymond C. Stevens et al.   NATURE REVIEWS DRUG DISCOVERY

Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series

(2011) Scott D. Kuduk et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

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

(2011) Carrie K Jones et al.   NEUROPSYCHOPHARMACOLOGY

Structural Determinants of Allosteric Agonism and Modulation at the M4Muscarinic Acetylcholine Receptor

(2010) Vindhya Nawaratne et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery and Characterization of Novel Subtype-Selective Allosteric Agonists for the Investigation of M1 Receptor Function in the Central Nervous System

(2009) Evan P Lebois et al.   ACS Chemical Neuroscience

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

Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties

(2009) Katie Leach et al.   NEUROPSYCHOPHARMACOLOGY

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

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

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

Mutagenic Mapping Suggests a Novel Binding Mode for Selective Agonists of M1 Muscarinic Acetylcholine Receptors

(2008) G. Lebon et al.   MOLECULAR PHARMACOLOGY

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

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