An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism

• Published in: Nature communications Vol. 14; no. 1; pp. 5938 - 12
• Main Authors: Lees, Joshua A., Dias, João M., Rajamohan, Francis, Fortin, Jean-Philippe, O’Connor, Rebecca, Kong, Jimmy X., Hughes, Emily A. G., Fisher, Ethan L., Tuttle, Jamison B., Lovett, Gabrielle, Kormos, Bethany L., Unwalla, Rayomand J., Zhang, Lei, Dechert Schmitt, Anne-Marie, Zhou, Dahui, Moran, Michael, Stevens, Kimberly A., Fennell, Kimberly F., Varghese, Alison E., Maxwell, Andrew, Cote, Emmaline E., Zhang, Yuan, Han, Seungil
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 23.09.2023; Nature Publishing Group; Nature Portfolio
• Subjects: 101/28; 631/45/612/194; 631/535/1258/1259; Agonists; Allosteric properties; Appetite; Binding sites; Body weight; Cachexia; Disorders; G protein-coupled receptors; Humanities and Social Sciences; Inverse agonists; Mode of action; multidisciplinary; Obesity; Phenotypes; Proteins; Receptors; Science; Science (multidisciplinary); Structural analysis; Structure-function relationships

GPR61 is an orphan GPCR related to biogenic amine receptors. Its association with phenotypes relating to appetite makes it of interest as a druggable target to treat disorders of metabolism and body weight, such as obesity and cachexia. To date, the lack of structural information or a known biologic...