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High-throughput screening campaign identifies a small molecule agonist of the relaxin family peptide receptor 4

  
@article{APS10211,
	author = {Guang-yao Lin and Lin Lin and Xiao-qing Cai and An-tao Dai and Yue Zhu and Jie Li and Qing Liu and De-hua Yang and Ross A. D. Bathgate and Ming-wei Wang},
	title = {High-throughput screening campaign identifies a small molecule agonist of the relaxin family peptide receptor 4},
	journal = {Acta Pharmacologica Sinica},
	volume = {41},
	number = {10},
	year = {2020},
	keywords = {},
	abstract = {Relaxin/insulin-like family peptide receptor 4 (RXFP4) is a class A G protein-coupled receptor (GPCR), and insulin-like peptide 5 (INSL5) is its endogenous ligand. Although the precise physiological role of INSL5/RXFP4 remains elusive, a number of studies have suggested it to be a potential therapeutic target for obesity and other metabolic disorders. Since selective agonists of RXFP4 are scarcely available and peptidic analogs of INSL5 are hard to make, we conducted a high-throughput screening campaign against 52,000 synthetic and natural compounds targeting RXFP4. Of the 109 initial hits discovered, only 3 compounds were confirmed in secondary screening, with JK0621-D008 displaying the best agonism at human RXFP4. Its S- configuration stereoisomer (JK1) was subsequently isolated and validated by a series of bioassays, demonstrating a consistent agonistic effect in cells overexpressing RXFP4. This scaffold may provide a valuable tool to further explore the biological functions of RXFP4.},
	url = {http://www.chinaphar.com/article/view/10211}
}