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Biochem Pharmacol

Title:		G protein-coupled receptors expressed and studied in yeast. The adenosine receptor as a prime example
Author(s):		Wang X; van Westen GJP; Heitman LH; AP IJ;
Address:		"Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Einsteinweg 55, 2333 CC Leiden, The Netherlands. Drug Discovery and Safety, Leiden Academic Centre for Drug Research, Einsteinweg 55, 2333 CC Leiden, The Netherlands; Oncode Institute, Leiden, The Netherlands"
Journal Title:		Biochem Pharmacol
Year:		2021
Volume:		20201216
Issue:
Page Number:		114370 -
DOI:		10.1016/j.bcp.2020.114370
ISSN/ISBN:		1873-2968 (Electronic) 0006-2952 (Linking)
Abstract:		"G protein-coupled receptors (GPCRs) are the largest class of membrane proteins with around 800 members in the human genome/proteome. Extracellular signals such as hormones and neurotransmitters regulate various biological processes via GPCRs, with GPCRs being the bodily target of 30-40% of current drugs on the market. Complete identification and understanding of GPCR functionality will provide opportunities for novel drug discovery. Yeast expresses three different endogenous GPCRs regulating pheromone and sugar sensing, with the pheromone pathway offering perspectives for the characterization of heterologous GPCR signaling. Moreover, yeast offers a ''null' background for studies on mammalian GPCRs, including GPCR activation and signaling, ligand identification, and characterization of disease-related mutations. This review focuses on modifications of the yeast pheromone signaling pathway for functional GPCR studies, and on opportunities and usage of the yeast system as a platform for human GPCR studies. Finally, this review discusses in some further detail studies of adenosine receptors heterologously expressed in yeast, and what Geoff Burnstock thought of this approach"
Keywords:		"Adenosine A2 Receptor Agonists/pharmacology Adenosine A2 Receptor Antagonists/pharmacology Animals *Gene Expression Regulation, Fungal Humans Protein Engineering/methods Purinergic P1 Receptor Agonists/pharmacology Purinergic P1 Receptor Antagonists/pharm;"
Notes:		"MedlineWang, Xuesong van Westen, Gerard J P Heitman, Laura H IJzerman, Adriaan P eng Research Support, Non-U.S. Gov't Review England 2020/12/19 Biochem Pharmacol. 2021 May; 187:114370. doi: 10.1016/j.bcp.2020.114370. Epub 2020 Dec 16"