Metabotropic glutamate receptor 4
Mammalian protein found in humans
Metabotropic glutamate receptor 4 is a protein that in humans is encoded by the GRM4 gene.
Together with GRM6, GRM7 and GRM8 it belongs to group III of the metabotropic glutamate receptor family. Group III receptors are linked to the inhibition of the cyclic AMP cascade. Activation of GRM4 has potential therapeutic benefits in the treatment of parkinson's disease. Splice variant "taste-GRM4" is involved in the perception of umami taste.
01Ligands
Orthosteric
- Cinnabarinic acid, a tryptophan metabolite
- LSP1-2111: agonist
- LSP4-2022: agonist
- LSP2-9166: mixed agonist at mGluR4 and mGluR7
Positive allosteric modulators (PAMs)
- ADX88178
- Foliglurax (PXT-002331, DT-1687)
- Tricyclic thiazolopyrazole derivative 22a: EC50 = 9 nM, Emax = 120%
- ML-128: EC50 = 240 nM, Emax = 182%
- Valiglurax (AP-472) (VU0652957)
- VU-0418506
- VU-001171: EC50 = 650 nM, Emax = 141%, 36-fold shift
- VU0155041: subtype-selective PAM, intrinsic allosteric agonist activity, robust in-vivo activity
- VU0364770
- PHCCC: PAM of mGluR4, negative allosteric modulator of mGluR1, direct agonist at mGluR6
- TC-N 22A
Sources and credits
This article is adapted from the Wikipedia article “Metabotropic glutamate receptor 4”, written by its contributors and licensed under CC BY-SA 4.0. Fathomly has changed the layout, removed citation markers, navigation and maintenance notices, and adjusted punctuation. This adapted version is shared under the same license. For references, see the original article.
Images, from Wikimedia Commons:
- Ideogram human chromosome 6.svg by National Center for Biotechnology Information, U.S. National Library of Medicine, Public domain
Fathomly is not affiliated with or endorsed by the Wikimedia Foundation. Spotted a problem? Tell us.