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Title: Design, synthesis and characterization of a new series of fluorescent metabotropic glutamate receptor type 5 negative allosteric modulators
Author: Fernández Dueñas, Víctor
Qian, Mingcheng
Argerich, Josep
Amaral, Carolina
Risseeuw, Martijn D.P.
Van Calenbergh, Serge
Ciruela Alférez, Francisco
Keywords: Enzims al·lostèrics
Allosteric enzymes
Issue Date: 1-Apr-2020
Publisher: MDPI
Abstract: In recent years, new drug discovery approaches based on novel pharmacological concepts have emerged. Allosteric modulators, for example, target receptors at sites other than the orthosteric binding sites and can modulate agonist-mediated activation. Interestingly, allosteric regulation may allow a fine-tuned regulation of unbalanced neurotransmitter' systems, thus providing safe and effective treatments for a number of central nervous system diseases. The metabotropic glutamate type 5 receptor (mGlu5R) has been shown to possess a druggable allosteric binding domain. Accordingly, novel allosteric ligands are being explored in order to finely regulate glutamate neurotransmission, especially in the brain. However, before testing the activity of these new ligands in the clinic or even in animal disease models, it is common to characterize their ability to bind mGlu5Rs in vitro. Here, we have developed a new series of fluorescent ligands that, when used in a new NanoBRET-based binding assay, will facilitate screening for novel mGlu5R allosteric modulators.
Note: Reproducció del document publicat a:
It is part of: Molecules, 2020, vol. 25, num. 7, p. 1532
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ISSN: 1420-3049
Appears in Collections:Articles publicats en revistes (Patologia i Terapèutica Experimental)
Articles publicats en revistes (Institut d'lnvestigació Biomèdica de Bellvitge (IDIBELL))

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