期刊
MOLECULES
卷 25, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/molecules25071532
关键词
mGlu(5)R; fluorescent ligands; allosterism; nanoBRET
资金
- FEDER/Ministerio de Ciencia, Innovacion y Universidades-Agencia Estatal de Investigacion [SAF2017-87349-R]
- ISCIII [PIE14/00034]
- Catalan government [2017 SGR 1604]
- Fundacio la Marato de TV3 [20152031]
- FWO [SBO-140028]
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 (mGlu(5)R) 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 mGlu(5)Rs 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 mGlu(5)R allosteric modulators.
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