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Neuropharmacology. 2015 Oct;97:142-8 doi: 10.1016/j.neuropharm.2015.05.017. 2015 May 27.

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

Poutiainen P, Kil KE, Zhang Z, Kuruppu D, Tannous B, Brownell AL.

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.

PMID: 26025660
| MGH/HST Martinos Center for Biomedical Imaging

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