Literature DB >> 29057037

Anti-inflammatory Silent Agonists.

Nicole A Horenstein1, Roger L Papke2.   

Abstract

The traditional view of nicotinic acetylcholine receptors (nAChRs) is that they strictly exert their functions via their well-known ion channel activity. With the identification of the cholinergic anti-inflammatory pathway and the critical involvement of the α7 nAChR, an alternate modality of function has emerged for the receptor involving metabotropic-like activity. The new emerging pharmacology for the receptor includes ligands termed silent agonists, which exert little or no ionotropic activity, yet are capable of modulating cellular inflammatory responses.

Year:  2017        PMID: 29057037      PMCID: PMC5641964          DOI: 10.1021/acsmedchemlett.7b00368

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN: 1948-5875            Impact factor:   4.345


  14 in total

1.  Stimulation of the vagus nerve attenuates macrophage activation by activating the Jak2-STAT3 signaling pathway.

Authors:  Wouter J de Jonge; Esmerij P van der Zanden; Frans O The; Maarten F Bijlsma; David J van Westerloo; Roelof J Bennink; Hans-Rudolf Berthoud; Satoshi Uematsu; Shizuo Akira; Rene M van den Wijngaard; Guy E Boeckxstaens
Journal:  Nat Immunol       Date:  2005-07-17       Impact factor: 25.606

Review 2.  Physiology and immunology of the cholinergic antiinflammatory pathway.

Authors:  Kevin J Tracey
Journal:  J Clin Invest       Date:  2007-02       Impact factor: 14.808

Review 3.  Non-canonical Signaling, the Hidden Life of Ligand-Gated Ion Channels.

Authors:  Sergio Valbuena; Juan Lerma
Journal:  Neuron       Date:  2016-10-19       Impact factor: 17.173

Review 4.  Looking below the surface of nicotinic acetylcholine receptors.

Authors:  Clare Stokes; Millet Treinin; Roger L Papke
Journal:  Trends Pharmacol Sci       Date:  2015-06-08       Impact factor: 14.819

5.  Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor.

Authors:  Kinga Chojnacka; Roger L Papke; Nicole A Horenstein
Journal:  Bioorg Med Chem Lett       Date:  2013-05-23       Impact factor: 2.823

6.  The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor.

Authors:  Roger L Papke; Deniz Bagdas; Abhijit R Kulkarni; Timothy Gould; Shakir D AlSharari; Ganesh A Thakur; M Imad Damaj
Journal:  Neuropharmacology       Date:  2014-12-11       Impact factor: 5.250

7.  The minimal pharmacophore for silent agonism of the α7 nicotinic acetylcholine receptor.

Authors:  Roger L Papke; Kinga Chojnacka; Nicole A Horenstein
Journal:  J Pharmacol Exp Ther       Date:  2014-07-02       Impact factor: 4.030

8.  The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia.

Authors:  Morten S Thomsen; Jens D Mikkelsen
Journal:  J Neuroimmunol       Date:  2012-08-09       Impact factor: 3.478

Review 9.  Anti-inflammatory role of microglial alpha7 nAChRs and its role in neuroprotection.

Authors:  Javier Egea; Izaskun Buendia; Esther Parada; Elisa Navarro; Rafael León; Manuela G Lopez
Journal:  Biochem Pharmacol       Date:  2015-07-29       Impact factor: 5.858

10.  X-ray structure of the human α4β2 nicotinic receptor.

Authors:  Claudio L Morales-Perez; Colleen M Noviello; Ryan E Hibbs
Journal:  Nature       Date:  2016-10-03       Impact factor: 49.962

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  18 in total

1.  Macroscopic and Microscopic Activation of α7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107.

Authors:  Marta Quadri; Sumanta Garai; Ganesh A Thakur; Clare Stokes; Alican Gulsevin; Nicole A Horenstein; Roger L Papke
Journal:  Mol Pharmacol       Date:  2018-10-22       Impact factor: 4.436

2.  Allosteric Agonism of α7 Nicotinic Acetylcholine Receptors: Receptor Modulation Outside the Orthosteric Site.

Authors:  Alican Gulsevin; Roger L Papke; Clare Stokes; Sumanta Garai; Ganesh A Thakur; Marta Quadri; Nicole A Horenstein
Journal:  Mol Pharmacol       Date:  2019-04-03       Impact factor: 4.436

3.  A Computational Analysis of the Factors Governing the Dynamics of α7 nAChR and Its Homologs.

Authors:  Alican Gulsevin; Jens Meiler; Nicole A Horenstein
Journal:  Biophys J       Date:  2020-09-16       Impact factor: 4.033

4.  Functional α7 nicotinic acetylcholine receptors in GABAergic neurons of the interpeduncular nucleus.

Authors:  Xiao-Tao Jin; Ryan M Drenan
Journal:  Neuropharmacology       Date:  2022-02-12       Impact factor: 5.250

5.  Allosterically Potentiated α7 Nicotinic Acetylcholine Receptors: Reduced Calcium Permeability and Current-Independent Control of Intracellular Calcium.

Authors:  Douglas R Miller; Habibeh Khoshbouei; Sumanta Garai; Lucas N Cantwell; Clare Stokes; Ganesh Thakur; Roger L Papke
Journal:  Mol Pharmacol       Date:  2020-10-05       Impact factor: 4.436

6.  Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.

Authors:  Maria Chiara Pismataro; Nicole A Horenstein; Clare Stokes; Marta Quadri; Marco De Amici; Roger L Papke; Clelia Dallanoce
Journal:  Eur J Med Chem       Date:  2020-07-28       Impact factor: 6.514

7.  Stable desensitization of α7 nicotinic acetylcholine receptors by NS6740 requires interaction with S36 in the orthosteric agonist binding site.

Authors:  Maria Chiara Pismataro; Nicole A Horenstein; Clare Stokes; Clelia Dallanoce; Ganesh A Thakur; Roger L Papke
Journal:  Eur J Pharmacol       Date:  2021-05-15       Impact factor: 5.195

Review 8.  In Silico Modeling of the α7 Nicotinic Acetylcholine Receptor: New Pharmacological Challenges Associated with Multiple Modes of Signaling.

Authors:  Alican Gulsevin; Roger L Papke; Nicole Horenstein
Journal:  Mini Rev Med Chem       Date:  2020       Impact factor: 3.862

Review 9.  Cholinergic Modulation of Neuroinflammation: Focus on α7 Nicotinic Receptor.

Authors:  Roberta Piovesana; Michael Sebastian Salazar Intriago; Luciana Dini; Ada Maria Tata
Journal:  Int J Mol Sci       Date:  2021-05-06       Impact factor: 5.923

Review 10.  Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors.

Authors:  Roger L Papke; Nicole A Horenstein
Journal:  Pharmacol Rev       Date:  2021-07       Impact factor: 18.923

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