Glycine Receptor Drug Discovery

Advances in Pharmacology
Joseph W LynchArgel Estrada-Mondragon

Abstract

Postsynaptic glycine receptor (GlyR) chloride channels mediate inhibitory neurotransmission in the spinal cord and brain stem, although presynaptic and extrasynaptic GlyRs are expressed more widely throughout the brain. In humans, GlyRs are assembled as homo- or heteromeric pentamers of α1-3 and β subunits. GlyR malfunctions have been linked to a range of neurological disorders including hyperekplexia, temporal lobe epilepsy, autism, breathing disorders, and chronic inflammatory pain. Although it is possible that GlyRs may eventually be clinically targeted for a variety of neurological disorders, most research to date has focused on developing GlyR-targeted treatments for chronic pain. Inflammatory pain sensitization is caused by inflammatory mediators downregulating the magnitude of α3 GlyR-mediated inhibitory postsynaptic currents in spinal nociceptive neurons. Consistent with this paradigm, it is now well established that the selective enhancement of α3 GlyR current magnitude is effective in alleviating inflammatory pain. In this review, we briefly describe the physiological roles and pharmacological properties of GlyRs. We then outline the methods commonly used to discover new GlyR-active compounds and review recent progres...Continue Reading

Citations

Jul 20, 2018·Cell Biology International·Iryna LushnikovaGalyna Skibo
Mar 13, 2020·Bioinformatics·Adrien H CerdanMarco Cecchini
Jan 10, 2020·Annual Review of Pharmacology and Toxicology·Kazuhiko MatsudaDavid B Sattelle
Apr 24, 2020·Frontiers in Neuroscience·Bettina U WilkeMichaela Kress
Dec 19, 2020·International Journal of Molecular Sciences·Tomoya Kitayama
May 8, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Nawid MadjrohAnders A Jensen
Jul 3, 2021·Biomolecules·Hanns Ulrich ZeilhoferGonzalo E Yévenes
Jun 16, 2021·Biochemical Pharmacology·R NeffD Bertrand
Dec 2, 2020·Journal of Chemical Information and Modeling·Pilar A VásquezLeonardo Guzmán
Mar 21, 2019·ACS Chemical Neuroscience·Cesar O LaraGustavo Moraga-Cid
Sep 25, 2021·Biochemical Pharmacology·Nawid MadjrohAnders A Jensen

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