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index medicus (66) 66
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1. Full Text Discovery, synthesis and characterization of a highly mAChR selective M5 orthosteric antagonist, VU0488130 (ML381): a novel molecular probe
by Gentry, Patrick R and Kokubo, Masaya and Bridges, Thomas M and Cho, Hyekyung P and Smith, Emery and Chase, Peter and Hodder, Peter S and Utley, Thomas J and Rajapakse, Anuruddha and Byers, Frank and Niswender, Colleen M and Morrison, Ryan D and Daniels, J. Scott and Wood, Michael R and Conn, P. Jeffrey and Lindsley, Craig W
ChemMedChem, ISSN 1860-7179, 8/2014, Volume 9, Issue 8, pp. 1677 - 1682
Of the five G-protein-coupled muscarinic acetylcholine receptors (mAChRs or M 1 -M 5 ), M 5 is the least explored and understood due to a lack of mAChR subtype... 
muscarinic | acetylcholine | antagonist | orthosteric
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2. Full Text Aiming for allosterism: Evaluation of allosteric modulators of CB 1 in a neuronal model
by Straiker, Alex and Mitjavila, José and Yin, Danielle and Gibson, Anne and Mackie, Ken
Pharmacological Research, ISSN 1043-6618, 07/2015, Volume 99, pp. 370 - 376
Cannabinoid pharmacology has proven nettlesome with issues of promiscuity a common theme among both agonists and antagonists. One recourse is to develop... 
Allosteric | Depolarization-induced suppression of excitation | Excitatory postsynaptic current | Allosterism | Orthosteric | Cannabinoid | Tetrahydrocannabinol
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3. Full Text Molecular exploration of the α1A-adrenoceptor orthosteric site: Binding site definition for epinephrine, HEAT and prazosin
by Maïga, Arhamatoulaye and Dupont, Mélanie and Blanchet, Guillaume and Marcon, Elodie and Gilquin, Bernard and Servent, Denis and Gilles, Nicolas
FEBS Letters, ISSN 0014-5793, 12/2014, Volume 588, Issue 24, pp. 4613 - 4619
Despite the physiological and pharmacological importance of the α -adrenoreceptor, the mode of interactions of classical agonists and radioactive ligands with... 
Epinephrine | HEAT | Prazosin | Binding study | Adrenoceptor | Orthosteric site
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4. Full Text Chemical Modification of the M1 Agonist VU0364572 Reveals Molecular Switches in Pharmacology and a Bitopic Binding Mode
by Digby, Gregory J and Utley, Thomas J and Lamsal, Atin and Sevel, Christian and Sheffler, Douglas J and Lebois, Evan P and Bridges, Thomas M and Wood, Michael R and Niswender, Colleen M and Lindsley, Craig W and Conn, P. Jeffrey
ACS Chemical Neuroscience, ISSN 1948-7193, 09/2012, Volume 3, Issue 12, pp. 1025 - 1036
We previously reported the discovery of VU0364572 and VU0357017 as M1-selective agonists that appear to activate M1 through actions at an allosteric site.... 
GPCR | allosteric | Acetylcholine | agonist | antagonist | orthosteric
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5. Full Text Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R)
by Kumar, Vivek and Moritz, Amy E and Keck, Thomas M and Bonifazi, Alessandro and Ellenberger, Michael P and Sibley, Christopher D and Free, R. Benjamin and Shi, Lei and Lane, J. Robert and Sibley, David R and Newman, Amy Hauck
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2017, Volume 60, Issue 4, pp. 1478 - 1494
The development of bitopic ligands directed toward D2-like receptors has proven to be of particular interest to improve the selectivity and/or affinity of... 
synthon | dopamine D2 receptor | β-arrestin | secondary pharmacophore | orthosteric binding site | primary pharmacophore | bitopic ligand | cyclopropyl | antagonist | dopamine D3 receptor | allosteric modulator
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6. Full Text Towards understanding the structural basis of partial agonism at the dopamine D3 receptor
by Michino, Mayako and Boateng, Comfort A and Donthamsetti, Prashant and Yano, Hideaki and Bakare, Oluyomi M and Bonifazi, Alessandro and Ellenberger, Michael P and Keck, Thomas M and Kumar, Vivek and Zhu, Clare and Verma, Ravi and Deschamps, Jeffrey R and Javitch, Jonathan A and Newman, Amy Hauck and Shi, Lei
Journal of medicinal chemistry, ISSN 0022-2623, 1/2017, Volume 60, Issue 2, pp. 580 - 593
Both dopamine D 3 receptor (D 3 R) partial agonists and antagonists have been implicated as potential medications for substance use disorders. In contrast to... 
synthon | partial agonist | Dopamine D3 receptor | orthosteric binding site | molecular dynamics | antagonist | phenylpiperazine
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7. Development of radioligands for the imaging of α7 nicotinic acetylcholine receptors with positron emission tomography
by Brust, Peter and Peters, Dan and Deuther-Conrad, Winnie
Current Drug Targets, ISSN 1389-4501, 05/2012, Volume 13, Issue 5, pp. 594 - 601
Molecular imaging | Drug design | Neurodegeneration | Orthosteric ligand | Nicotine
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8. Full Text Combined effects of mutations in loop C and the loop D-E-G triangle on neonicotinoid interactions with Drosophila Dα1/chicken β2 hybrid nAChRs
by Hikida, Mai and Shimada, Shota and Kurata, Ryo and Shigetou, Sho and Ihara, Makoto and Sattelle, David B and Matsuda, Kazuhiko
Pesticide Biochemistry and Physiology, ISSN 0048-3575, 10/2018, Volume 151, pp. 47 - 52
Neonicotinoid insecticides interact with the orthosteric sites of nicotinic acetylcholine receptors (nAChRs) formed at the interfaces of (a) two adjacent α... 
Neonicotinoid | Imidacloprid | Orthosteric binding site | Thiacloprid | Nicotinic acetylcholine receptor | α subunit
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9. Full Text Discovery and Development of Muscarinic Acetylcholine M4 Activators as Promising Therapeutic Agents for CNS Diseases
by Kentaro Takai and Takeshi Enomoto and Sumitomo Dainippon Pharma Co and Drug Research Division and Ltd
Chemical and Pharmaceutical Bulletin, ISSN 0009-2363, 2018, Volume 66, Issue 1, pp. 37 - 44
Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of... 
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10. Molecular Basis of Modulating Adenosine Receptors Activities
by Al-Qattan, MNM and Mordi, MN
CURRENT PHARMACEUTICAL DESIGN, ISSN 1381-6128, 2019, Volume 25, Issue 7, pp. 817 - 831
Modulating cellular processes through extracellular chemical stimuli is medicinally an attractive approach to control disease conditions. GPCRs are the most... 
LIGAND-BINDING | 2ND EXTRACELLULAR LOOP | interaction model | SITE-DIRECTED MUTAGENESIS | allosteric ligands | A RECEPTOR | BIASED AGONISM | ALLOSTERIC COMMUNICATION PIPELINES | PROTEIN-COUPLED RECEPTOR | STRUCTURAL BASIS | GPCR | FUNCTIONAL SELECTIVITY | PHARMACOLOGY & PHARMACY | Adenosine receptor | receptor conformations | A(2A) RECEPTOR | modulators | orthosteric
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11. Full Text Effects mediated by M2 muscarinic orthosteric agonist on cell growth in human neuroblastoma cell lines
by Lucianò, Anna Maria and Mattei, Francesca and Damo, Elisa and Panzarini, Elisa and Dini, Luciana and Tata, Ada Maria
Pure and Applied Chemistry, ISSN 0033-4545, 2019, Volume 91, Issue 10, pp. 1641 - 1650
The role of muscarinic receptors has been largely documented over the past few decades. Recently we demonstrated that the activation of M2 muscarinic receptors... 
neuroblastoma | orthosteric ligand | cell proliferation | Eurasia 2018 | M2 receptors | survival | RECEPTOR ACTIVATION | PROLIFERATION | CYCLE PROGRESSION | CHEMISTRY, MULTIDISCIPLINARY
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12. Full Text Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
by Penjišević, Jelena Z and Šukalović, Vladimir V and Andrić, Deana B and Roglić, Goran M and Novaković, Irena T and Šoškić, Vukić and Kostić-Rajačić, Sladana V
Journal of the Serbian Chemical Society, ISSN 0352-5139, 2016, Volume 81, Issue 4, pp. 347 - 356
A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates... 
Allosteric | Dopamine D | receptor | Docking analysis | Orthosteric binding site | Docking | Dopamine | Synthesis | allosteric | dopamine D2 receptor | orthosteric bind site | docking analysis
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13. Full Text The Structural Binding Mode of the Four Autotaxin Inhibitor Types that Differentially Affect Catalytic and Non-Catalytic Functions
by Salgado-Polo, Fernando and Perrakis, Anastassis
Cancers, ISSN 2072-6694, 10/2019, Volume 11, Issue 10, p. 1577
Autotaxin (ATX) is a secreted lysophospholipase D, catalysing the conversion of lysophosphatidylcholine (LPC) to bioactive lysophosphatidic acid (LPA). LPA... 
allosteric | lysophosphatidic acid | inhibitor | autotaxin | gpcr | orthosteric | lipid chaperone | signalling
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14. Full Text Extracellular calcium modulates actions of orthosteric and allosteric ligands on metabotropic glutamate receptor 1α
by Jiang, Jason Y and Nagaraju, Mulpuri and Meyer, Rebecca C and Zhang, Li and Hamelberg, Donald and Hall, Randy A and Brown, Edward M and Conn, P. Jeffrey and Yang, Jenny J
Journal of Biological Chemistry, ISSN 0021-9258, 01/2014, Volume 289, Issue 3, pp. 1649 - 1661
Background: Extracellular Ca2+ alters mGluR1 activity but by an unknown mechanism. Results: Mutations in predicted Ca2+-binding sites modulated the potency of... 
MOLECULAR-MECHANISM | G Protein-coupled Receptors (GPCR) | Allosteric Modulators | DOMAIN | ACTIVATION | ANTAGONIST | Calcium | CPCCOET | BIOCHEMISTRY & MOLECULAR BIOLOGY | Calcium-binding Proteins | Orthosteric Antagonist | IDENTIFICATION | Drug Discovery | STRUCTURAL BASIS | CA2 | CA2+-BINDING SITES | BINDING-SITE | Glutamate Receptors Metabotropic | Orthosteric Agonist | Allosteric Regulation - drug effects | Protein Structure, Tertiary | Glycine - analogs & derivatives | Allosteric Regulation - genetics | Benzoates | Calcium - metabolism | Calcium Signaling - physiology | Humans | Excitatory Amino Acid Agonists - pharmacology | Receptors, Metabotropic Glutamate - metabolism | Mutation, Missense | Receptors, Metabotropic Glutamate - genetics | Calcium Signaling - drug effects | HEK293 Cells | Receptors, Metabotropic Glutamate - agonists | Binding Sites | Receptors, Metabotropic Glutamate - antagonists & inhibitors | Xanthenes - pharmacology | Amino Acid Substitution | Carbamates - pharmacology | Quisqualic Acid - pharmacology | Molecular Biophysics
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15. Full Text Enantiomer-specific positive allosteric modulation of CB1 signaling in autaptic hippocampal neurons
by Mitjavila, Jose and Yin, Danielle and Kulkarni, Pushkar M and Zanato, Chiara and Thakur, Ganesh A and Ross, Ruth and Greig, Iain and Mackie, Ken and Straiker, Alex
Pharmacological Research, ISSN 1043-6618, 03/2018, Volume 129, pp. 475 - 481
The cannabinoid signaling system is found throughout the CNS and its involvement in several pathological processes makes it an attractive therapeutic target.... 
Allosteric | G protein-coupled receptor | CB1 | Cannabinoid receptor | Orthosteric | TRANSMISSION | PROTEIN | RECEPTOR | PHARMACOLOGY & PHARMACY | cannabinoid receptor | orthosteric
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16. Full Text Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2
by Doornbos, Maarten L.J and Vermond, Sophie C and Lavreysen, Hilde and Tresadern, Gary and IJzerman, Adriaan P and Heitman, Laura H
Biochemical Pharmacology, ISSN 0006-2952, 09/2018, Volume 155, pp. 356 - 365
While many orthosteric ligands have been developed for the mGlu receptor, little is known about their target binding kinetics and how these relate to those of... 
Binding kinetics | Glutamate | Allosteric modulation | Orthosteric | mGlu2 receptor | mGlu | receptor | MOLECULAR-MECHANISM | EFFICACY | PHARMACOLOGICAL CHARACTERIZATION | DRUG DISCOVERY | PROTEIN-COUPLED RECEPTORS | MUSCARINIC M-3 RECEPTOR | MAJOR DEPRESSION | TARGET BINDING | mGlu receptor | PHARMACOLOGY & PHARMACY | RAT-BRAIN | MGLU2 RECEPTOR | Amino acids | Drug discovery
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17. Full Text Targeting protein-protein interaction by small molecules
by Jin, Lingyan and Wang, Weiru and Fang, Guowei
Annual Review of Pharmacology and Toxicology, ISSN 0362-1642, 2014, Volume 54, Issue 1, pp. 435 - 456
Protein-protein interactions (PPIs) are critical regulatory events in physiology and pathology, and they represent an important target space for... 
Allosteric inhibitors | Interfacial binders | Orthosteric inhibitors | Small-molecule inhibitors | Protein-protein interactions | PPIs | interfacial binders | PYRUVATE-KINASE M2 | DRUG DISCOVERY | protein-protein interactions | AGGRESSIVE CARCINOMA | SIGNAL-TRANSDUCTION | STRUCTURAL BASIS | IN-VIVO | NUCLEOTIDE EXCHANGE FACTOR | CANCER METABOLISM | PHARMACOLOGY & PHARMACY | allosteric inhibitors | BREFELDIN-A | TOXICOLOGY | orthosteric inhibitors | B-RAF | small-molecule inhibitors | SOS1 Protein - antagonists & inhibitors | ras Proteins - genetics | Humans | ras Proteins - metabolism | Molecular Targeted Therapy | Proto-Oncogene Proteins c-akt - genetics | Carrier Proteins - agonists | SOS1 Protein - genetics | Membrane Proteins - metabolism | Proto-Oncogene Proteins c-akt - metabolism | Proto-Oncogene Proteins B-raf - metabolism | Protein Interaction Domains and Motifs - drug effects | Membrane Proteins - genetics | SOS1 Protein - metabolism | ras Proteins - antagonists & inhibitors | Models, Molecular | Thyroid Hormones - agonists | Thyroid Hormones - genetics | Membrane Proteins - agonists | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Carrier Proteins - genetics | Carrier Proteins - metabolism | Proto-Oncogene Proteins B-raf - genetics | Thyroid Hormones - metabolism | Protein Binding | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | Proteins | Protein binding
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18. Full Text Characterization of methanthelinium binding and function at human M 1 –M 5 muscarinic acetylcholine receptors
by Irmen, Matthias and Holze, Janine and Bödefeld, Theresa and Tränkle, Christian
Naunyn-Schmiedeberg's Archives of Pharmacology, ISSN 0028-1298, 10/2018, Volume 391, Issue 10, pp. 1037 - 1052
Firstly, it was determined whether methanthelinium bromide (MB) binds to human M-1-M-5 (hM(1)-hM(5)) muscarinic acetylcholine receptors in comparison to the... 
Allosteric | Hyperhidrosis axillaris | Muscarinic receptor | NMS | Orthosteric | Methanthelinium bromide | SUBTYPE | SITE | RADIOLIGAND | ECCRINE SWEAT GLAND | MODULATORS | PROTEIN-COUPLED RECEPTORS | ALLOSTERIC LIGANDS | HYPERHIDROSIS | INHIBITION | PHARMACOLOGY & PHARMACY | ANTAGONISTS
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19. Full Text Neurochemical and behavioral studies on the 5-HT1A-dependent antipsychotic action of the mGlu(4) receptor agonist LSP4-2022
by Wozniak, M and Golembiowska, K and Noworyta-Sokolowska, K and Acher, F and Cieslik, P and Kusek, M and Tokarski, K and Pilc, A and Wieronska, JM
NEUROPHARMACOLOGY, ISSN 0028-3908, 03/2017, Volume 115, pp. 149 - 165
LSP4-2022 is a novel, orthosteric agonist of mGlu(4) receptor that induces antipsychotic-like activity in animal studies. In the present study, the involvement... 
Dopamine | Serotonin | PHENCYCLIDINE-INDUCED DOPAMINE | 5-HT1A RECEPTORS | Schizophrenia | SEROTONIN RELEASE | METABOTROPIC GLUTAMATE RECEPTORS | GROUP-III | Glutamate | NEUROSCIENCES | ORTHOSTERIC AGONIST | mGlu | IMMUNOCYTOCHEMICAL LOCALIZATION | PYRAMIDAL NEURONS | GABA | 5-HT1A | MEDIAL PREFRONTAL CORTEX | PHARMACOLOGY & PHARMACY | RAT-BRAIN
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20. Full Text Two PKA RI alpha holoenzyme states define ATP as an isoform-specific orthosteric inhibitor that competes with the allosteric activator, cAMP
by Lu, TW and Wu, J and Aoto, PC and Weng, JH and Ahuja, LG and Sun, N and Cheng, CY and Zhang, P and Taylor, SS
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, ISSN 0027-8424, 08/2019, Volume 116, Issue 33, pp. 16347 - 16356
Protein kinase A (PKA) holoenzyme, comprised of a cAMP-binding regulatory (R)-subunit dimer and 2 catalytic (C)-subunits, is the master switch for... 
CATALYTIC SUBUNIT | isoform-specific quaternary structure | CRYSTAL-STRUCTURE | MULTIDISCIPLINARY SCIENCES | DEPENDENT PROTEIN-KINASE | cAMP | STRUCTURE REVEALS | TARGETED DISRUPTION | I-ALPHA | allosteric and orthosteric regulation | SITE MUTATIONS DEFINE | structural biology | A REGULATORY SUBUNIT | protein kinase A | BETA-SUBUNIT | BINDING | Protein kinase A | Crosstalk | Cyclic AMP | Activation | Kinases | Substrates | Interfaces | Allosteric properties | Isoforms | Dimers | Catalysis | Magnesium | ATP
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