Literature DB >> 26025660

Co-operative binding assay for the characterization of mGlu4 allosteric modulators.

Pekka Poutiainen1, Kun-Eek Kil1, Zhaoda Zhang1, Darshini Kuruppu2, Bakhos Tannous3, Anna-Liisa Brownell4.   

Abstract

The interest in the role of metabotropic glutamate receptor 4 (mGlu4) in CNS related disorders has increased the need for methods to investigate the binding of allosteric drug candidates. Our aim is to present the first fully characterized in vitro binding assay of mGlu4 positive allosteric modulators (PAMs). Results suggest that mGlu4 PAMs have characteristic co-operative binding with orthosteric glutamate, which offers a notable insight to the further development of mGlu4 targeted therapies.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Binding affinity; Metabotropic glutamate receptor; Parkinson disease; mGlu(4)

Mesh：

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Year:  2015        PMID： 26025660      PMCID： PMC4537392          DOI： 10.1016/j.neuropharm.2015.05.017

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN： 0028-3908            Impact factor:   5.250


  26 in total

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  3 in total

1.  Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.

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Journal:  Mol Pharmacol       Date:  2018-03-15       Impact factor: 4.436

2.  Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.

Authors:  Zhaoda Zhang; Kun-Eek Kil; Pekka Poutiainen; Ji-Kyung Choi; Hye-Jin Kang; Xi-Ping Huang; Bryan L Roth; Anna-Liisa Brownell
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3.  Synthesis and Characterization of Fluorine-18-Labeled N-(4-Chloro-3-((fluoromethyl-d2)thio)phenyl)picolinamide for Imaging of mGluR4 in Brain.

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