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Recent advances in the drug discovery of metabotropic glutamate receptor 4 (mGluR4) activators for the treatment of CNS and non-CNS disorders

(Group Leader) & (Group Leader)
Pages 261-280 | Published online: 14 Feb 2012

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Anna Stankiewicz, Katarzyna Kaczorowska, Ryszard Bugno, Aneta Kozioł, Maria H. Paluchowska, Grzegorz Burnat, Barbara Chruścicka, Paulina Chorobik, Piotr Brański, Joanna M. Wierońska, Beata Duszyńska, Andrzej Pilc & Andrzej J. Bojarski. (2022) New 1,2,4-oxadiazole derivatives with positive mGlu4 receptor modulation activity and antipsychotic-like properties. Journal of Enzyme Inhibition and Medicinal Chemistry 37:1, pages 211-225.
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Dario Doller, Anton Bespalov, Rob Miller, Malgorzata Pietraszek & Mikhail Kalinichev. (2020) A case study of foliglurax, the first clinical mGluR4 PAM for symptomatic treatment of Parkinson’s disease: translational gaps or a failing industry innovation model?. Expert Opinion on Investigational Drugs 29:12, pages 1323-1338.
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Claudia Volpi, Francesca Fallarino, Giada Mondanelli, Antonio Macchiarulo & Ursula Grohmann. (2018) Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4. Expert Opinion on Drug Discovery 13:5, pages 411-423.
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Articles from other publishers (30)

Helena Domin. (2022) Group III metabotropic glutamate receptors as promising targets for neuroprotective therapy: Particular emphasis on the role of mGlu4 and mGlu7 receptors. Pharmacology Biochemistry and Behavior 219, pages 173452.
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Dario Doller. 2022. Comprehensive Pharmacology. Comprehensive Pharmacology 297 336 .
Lisha Zhou, Yingying Zhu, Wangyang Chen & Yiping Tang. (2021) Emerging role of microRNAs in major depressive disorder and its implication on diagnosis and therapeutic response. Journal of Affective Disorders 286, pages 80-86.
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Karen J. Gregory & Cyril Goudet. (2020) International Union of Basic and Clinical Pharmacology. CXI. Pharmacology, Signaling, and Physiology of Metabotropic Glutamate Receptors. Pharmacological Reviews 73:1, pages 521-569.
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Qi Zhang, Xinzhen Chen, Shanyawen Li, Ting Yao & Jing Wu. (2021) Association between the group III metabotropic glutamate receptor gene polymorphisms and attention-deficit/hyperactivity disorder and functional exploration of risk loci. Journal of Psychiatric Research 132, pages 65-71.
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Akriti Srivastava, Brati Das, Annie Y. Yao & Riqiang Yan. (2020) Metabotropic Glutamate Receptors in Alzheimer’s Disease Synaptic Dysfunction: Therapeutic Opportunities and Hope for the Future. Journal of Alzheimer's Disease 78:4, pages 1345-1361.
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Serena Boccella, Ida Marabese, Francesca Guida, Livio Luongo, Sabatino Maione & Enza Palazzo. (2019) The Modulation of Pain by Metabotropic Glutamate Receptors 7 and 8 in the Dorsal Striatum. Current Neuropharmacology 18:1, pages 34-50.
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Ilaria Dal Prà, Ubaldo Armato & Anna Chiarini. (2019) Family C G-Protein-Coupled Receptors in Alzheimer’s Disease and Therapeutic Implications. Frontiers in Pharmacology 10.
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Ana O. Pires, F.G. Teixeira, B. Mendes-Pinheiro, Sofia C. Serra, Nuno Sousa & António J. Salgado. (2017) Old and new challenges in Parkinson's disease therapeutics. Progress in Neurobiology 156, pages 69-89.
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Hassaan Mehboob Awan, Abdullah Shah, Farooq Rashid & Ge Shan. (2017) Primate-specific Long Non-coding RNAs and MicroRNAs. Genomics, Proteomics & Bioinformatics 15:3, pages 187-195.
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Nadhir Litim, Marc Morissette & Thérèse Di Paolo. (2017) Metabotropic glutamate receptors as therapeutic targets in Parkinson's disease: An update from the last 5 years of research. Neuropharmacology 115, pages 166-179.
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Claudia Volpi, Giada Mondanelli, Maria T. Pallotta, Carmine Vacca, Alberta Iacono, Marco Gargaro, Elisa Albini, Roberta Bianchi, Maria L. Belladonna, Sylvain Celanire, C?line Mordant, Madeleine Heroux, Isabelle Royer-Urios, Manfred Schneider, Pierre-Alain Vitte, Mathias Cacquevel, Laurent Galibert, Sonia-Maria Poli, Aldo Solari, Silvio Bicciato, Mario Calvitti, Cinzia Antognelli, Paolo Puccetti, Ciriana Orabona, Francesca Fallarino & Ursula Grohmann. (2016) Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells. Neuropharmacology 102, pages 59-71.
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Jing Li, Huaqing Meng, Wan Cao & Tian Qiu. (2015) MiR-335 is involved in major depression disorder and antidepressant treatment through targeting GRM4. Neuroscience Letters 606, pages 167-172.
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Kasper Harpsøe, Vignir Isberg, Benjamin G. Tehan, Dahlia Weiss, Angela Arsova, Fiona H. Marshall, Hans Bräuner-Osborne & David E. Gloriam. (2015) Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants. Scientific Reports 5:1.
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Barbara Chruścicka, Grzegorz Burnat, Piotr Brański, Paulina Chorobik, Tomasz Lenda, Marcin Marciniak & Andrzej Pilc. (2015) Tetracycline-Based System for Controlled Inducible Expression of Group III Metabotropic Glutamate Receptors. SLAS Discovery 20:3, pages 350-358.
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Francine Acher & Cyril Goudet. (2015) Therapeutic potential of group III metabotropic glutamate receptor ligands in pain. Current Opinion in Pharmacology 20, pages 64-72.
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Marianne Amalric. (2015) Targeting metabotropic glutamate receptors (mGluRs) in Parkinson's disease. Current Opinion in Pharmacology 20, pages 29-34.
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Xavier Rovira, Fanny Malhaire, Pauline Scholler, Jordi Rodrigo, Patricia Gonzalez‐Bulnes, Amadeu Llebaria, Jean‐Philippe Pin, Jesús Giraldo & Cyril Goudef. (2014) Overlapping binding sites drive allosteric agonism and positive cooperativity in type 4 metabotropic glutamate receptors. The FASEB Journal 29:1, pages 116-130.
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Mikhail Kalinichev, Emmanuel Le Poul, Christelle Boléa, Françoise Girard, Brice Campo, Massimiliano Fonsi, Isabelle Royer-Urios, Susan E. Browne, Jason M. Uslaner, Matthew J. Davis, Jacob Raber, Robert Duvoisin, Simon T. Bate, Ian J. Reynolds, Sonia Poli & Sylvain Celanire. (2014) Characterization of the Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 ADX88178 in Rodent Models of Neuropsychiatric Disorders. Journal of Pharmacology and Experimental Therapeutics 350:3, pages 495-505.
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Juan Pablo Lopez, Raymond Lim, Cristiana Cruceanu, Liam Crapper, Caroline Fasano, Benoit Labonte, Gilles Maussion, Jennie P Yang, Volodymyr Yerko, Erika Vigneault, Salah El Mestikawy, Naguib Mechawar, Paul Pavlidis & Gustavo Turecki. (2014) miR-1202 is a primate-specific and brain-enriched microRNA involved in major depression and antidepressant treatment. Nature Medicine 20:7, pages 764-768.
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Salma E El-Habashy, Alaa M Nazief, Chris E Adkins, Ming Ming Wen, Amal H El-Kamel, Ahmed M Hamdan, Amira S Hanafy, Tori O Terrell, Afroz S Mohammad, Paul R Lockman & Mohamed Ismail Nounou. (2014) Novel treatment strategies for brain tumors and metastases. Pharmaceutical Patent Analyst 3:3, pages 279-296.
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Claire J. Williams & David T. Dexter. (2014) Neuroprotective and symptomatic effects of targeting group III mGlu receptors in neurodegenerative disease. Journal of Neurochemistry 129:1, pages 4-20.
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Manuel Cajina, Megan Nattini, Dekun Song, Gennady Smagin, Erling B. Jørgensen, Gamini Chandrasena, Christoffer Bundgaard, Dorthe Bach Toft, Xinyan Huang, Francine Acher & Dario Doller. (2013) Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist. ACS Medicinal Chemistry Letters 5:2, pages 119-123.
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Hilary Highfield Nickols & P. Jeffrey Conn. (2014) Development of allosteric modulators of GPCRs for treatment of CNS disorders. Neurobiology of Disease 61, pages 55-71.
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Sylvain Célanire, Benjamin Perry, Robert Lutjens, Sonia Poli & Ian J. Reynolds. 2013. Emerging Drugs and Targets for Parkinson’s Disease. Emerging Drugs and Targets for Parkinson’s Disease 237 265 .
M. Amalric, S. Lopez, C. Goudet, G. Fisone, G. Battaglia, F. Nicoletti, J.-P. Pin & F.C. Acher. (2013) Group III and subtype 4 metabotropic glutamate receptor agonists: Discovery and pathophysiological applications in Parkinson's disease. Neuropharmacology 66, pages 53-64.
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Vattoly J. Majo, Jaya Prabhakaran, J. John Mann & J.S. Dileep Kumar. (2013) PET and SPECT tracers for glutamate receptors. Drug Discovery Today 18:3-4, pages 173-184.
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Emmanuel Le Poul, Christelle Boléa, Francoise Girard, Sonia Poli, Delphine Charvin, Brice Campo, Julien Bortoli, Abdhelak Bessif, Bin Luo, Amy Jo Koser, Lisa M. Hodge, Karen M. Smith, Anthony G. DiLella, Nigel Liverton, Fred Hess, Susan E. Browne & Ian J. Reynolds. (2012) A Potent and Selective Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator Improves Movement in Rodent Models of Parkinson's Disease. Journal of Pharmacology and Experimental Therapeutics 343:1, pages 167-177.
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Peter J. Flor & Francine C. Acher. (2012) Orthosteric versus allosteric GPCR activation: The great challenge of group-III mGluRs. Biochemical Pharmacology 84:4, pages 414-424.
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Hermogenes N. Jimenez, Kevin G. Liu, Sang-Phyo Hong, Michael S. Reitman, Michelle A. Uberti, Maria D. Bacolod, Manuel Cajina, Megan Nattini, Michael Sabio & Dar?o Doller. (2012) 4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators. Bioorganic & Medicinal Chemistry Letters 22:9, pages 3235-3239.
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