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Molecular insights into ligand recognition and G protein coupling of the neuromodulatory orphan receptor GPR139

16 Dec 2021

Abstract excerpt

The G protein-coupled receptor GPR139 is involved in neuromodulation, and one of its agonists is in clinical trials for the treatment of cognitive impairment and negative symptoms of schizophrenia. While GPR139 is a understudied ‘orphan’ receptor, it can be activated by the amino acids l -Trp, l -Phe 1 or α-Melanocyte-stimulating hormone (α-MSH) which is an endogenous agonist of melanocortin receptors. 2 , 3...

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PMID: 34916631
DOI: 10.1038/s41422-021-00591-w

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