Functional and structural perspectives on allosteric modulation of GPCRs.
暂无分享,去创建一个
[1] J. Wess,et al. Activation and allosteric modulation of a muscarinic acetylcholine receptor , 2013, Nature.
[2] Hualiang Jiang,et al. Structure of the CCR5 Chemokine Receptor–HIV Entry Inhibitor Maraviroc Complex , 2013, Science.
[3] P. Sexton,et al. Structural Determinants of Allosteric Agonism and Modulation at the M4 Muscarinic Acetylcholine Receptor , 2010, The Journal of Biological Chemistry.
[4] G. Kunos,et al. Dihydroergocryptine binding and α-adrenoreceptors in smooth muscle , 1979, Nature.
[5] P. Sexton,et al. Probe Dependence in the Allosteric Modulation of a G Protein-Coupled Receptor: Implications for Detection and Validation of Allosteric Ligand Effects , 2012, Molecular Pharmacology.
[6] N. Birdsall,et al. Modification of the binding properties of muscarinic receptors by gallamine. , 1983, Molecular pharmacology.
[7] M. Babu,et al. Molecular signatures of G-protein-coupled receptors , 2013, Nature.
[8] S. Urwyler,et al. diamine (GS39783) and Structurally Related Compounds: Novel Allosteric Enhancers of -Aminobutyric Acid B Receptor Function , 2003 .
[9] P. Sexton,et al. Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor. , 2012, Endocrinology.
[10] P. Sexton,et al. Allosteric Modulation of a Chemogenetically Modified G Protein-Coupled Receptor , 2013, Molecular Pharmacology.
[11] C. Langmead,et al. Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. , 2006, Trends in pharmacological sciences.
[12] C. Langmead. Determining allosteric modulator mechanism of action: integration of radioligand binding and functional assay data. , 2011, Methods in molecular biology.
[13] C. Langmead,et al. Quantitative Analysis Reveals Multiple Mechanisms of Allosteric Modulation of the mGlu5 Receptor in Rat Astroglia , 2011, Molecular Pharmacology.
[14] Arthur Christopoulos,et al. Bridging the gap: bitopic ligands of G-protein-coupled receptors. , 2013, Trends in pharmacological sciences.
[15] H. Lavreysen,et al. Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function , 2012, Molecular Pharmacology.
[16] T. Kenakin,et al. Is prenalterol (H133/80) really a selective beta 1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships. , 1980, The Journal of pharmacology and experimental therapeutics.
[17] P. Sexton,et al. Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor. , 2013, Journal of medicinal chemistry.
[18] P. Sexton,et al. The Role of Transmembrane Domain 3 in the Actions of Orthosteric, Allosteric, and Atypical Agonists of the M4 Muscarinic Acetylcholine Receptor , 2011, Molecular Pharmacology.
[19] Judy Lin,et al. Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. , 2010, Journal of medicinal chemistry.
[20] P. Sexton,et al. A Monod-Wyman-Changeux Mechanism Can Explain G Protein-coupled Receptor (GPCR) Allosteric Modulation* , 2011, The Journal of Biological Chemistry.
[21] P. Sexton,et al. Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. , 2007, Trends in pharmacological sciences.
[22] A. Kruse,et al. Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist , 2011, Nature.
[23] C. Langmead. Ligand properties and behaviours in an allosteric age. , 2012, Trends in pharmacological sciences.
[24] F. Ehlert. Analysis of Allosterism in Functional Assays , 2005, Journal of Pharmacology and Experimental Therapeutics.
[25] F. Gasparini,et al. The Non-competitive Antagonists 2-Methyl-6-(phenylethynyl)pyridine and 7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic Acid Ethyl Ester Interact with Overlapping Binding Pockets in the Transmembrane Region of Group I Metabotropic Glutamate Receptors* , 2000, The Journal of Biological Chemistry.
[26] Ali Jazayeri,et al. Structure of class B GPCR corticotropin-releasing factor receptor 1 , 2013, Nature.
[27] C. Bissantz,et al. Structural determinants of allosteric antagonism at metabotropic glutamate receptor 2: mechanistic studies with new potent negative allosteric modulators , 2011, British journal of pharmacology.
[28] P. Sexton,et al. Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties , 2010, Neuropsychopharmacology.
[29] A. Christopoulos,et al. Allosteric Modulation of the Cannabinoid CB1 Receptor , 2005, Molecular Pharmacology.
[30] Albert C. Pan,et al. Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs , 2013, Nature.
[31] J. M. Mathiesen,et al. Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB‐1893 and MPEP , 2003, British journal of pharmacology.
[32] Jens Meiler,et al. Probing the Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a “Molecular Switch” in PAM Pharmacology , 2013, Molecular Pharmacology.
[33] F. Gasparini,et al. CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. , 1999, Molecular pharmacology.
[34] D. Hall,et al. Modeling the functional effects of allosteric modulators at pharmacological receptors: an extension of the two-state model of receptor activation. , 2000, Molecular pharmacology.
[35] M. Mammen,et al. A Novel Multivalent Ligand That Bridges the Allosteric and Orthosteric Binding Sites of the M2 Muscarinic Receptor , 2007, Molecular Pharmacology.
[36] Arthur Christopoulos,et al. Signalling bias in new drug discovery: detection, quantification and therapeutic impact , 2012, Nature Reviews Drug Discovery.
[37] Arthur Christopoulos,et al. A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity , 2008, Journal of Biological Chemistry.
[38] U. Holzgrabe,et al. Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity , 2009, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
[39] J. Changeux,et al. ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL. , 1965, Journal of molecular biology.
[40] Arthur Christopoulos,et al. Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations , 2013, Proceedings of the National Academy of Sciences.