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

Pekka Poutiainen, Kun-Eek Kil, Zhaoda Zhang, Darshini Kuruppu, Bakhos Tannous, Anna-Liisa Brownell

Neuropharmacology 2015 Oct

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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.

Citation

Pekka Poutiainen, Kun-Eek Kil, Zhaoda Zhang, Darshini Kuruppu, Bakhos Tannous, Anna-Liisa Brownell. Co-operative binding assay for the characterization of mGlu4 allosteric modulators. Neuropharmacology. 2015 Oct;97:142-8