Methods of identifying candidate compounds of the human G protein-coupled receptor, GPR50, as modulators of body mass or adiposity

摘要

The present invention relates to methods of using a G protein-coupled receptor (GPCR) to screen one or more candidate compounds as a modulator of body mass or of adiposity or of percentage body fat in a subject or as a pharmaceutical agent for obesity and conditions related thereto. Inverse agonists and antagonists of the invention are useful as therapeutic agents for the prevention or treatment of obesity and conditions related thereto, including hypertension, insulin resistance, metabolic syndrome, Type 2 diabetes, dyslipidemia, atherosclerosis, coronary heart disease, and stroke. Agonists and partial agonists of the invention are useful as therapeutic agents for the prevention or treatment of disorders ameliorated by increasing body mass including, but not limited to, cachexia.

主权项

1. A method of identifying a candidate compound for the modulation of body mass or adiposity in a mammal, comprising the steps of:
(a) contacting the compound with a G protein-coupled receptor (GPCR) comprising an amino acid sequence having at least 80% identity to SEQ ID NO: 2; wherein the receptor couples to a G protein; (b) determining the ability of the compound to inhibit or stimulate functionality of the GPCR; and (c) identifying a compound that inhibits or stimulates functionality of the GPCR as a candidate compound for the modulation of body mass or adiposity in a mammal.