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G protein-coupled receptors (GPCRs) are the largest family of transmembrane receptors in humans. Over 800 GPCRs regulate the (patho)biology of every organ, tissue, and cell type. Consequently, GPCRs are the most prominent therapeutic targets in medicine. Although over 30% of current U.S. Food and Drug Administration-approved drugs target GPCR signaling, most receptors remain understudied and therapeutically underutilized. Challenges include an incomplete understanding of GPCR signaling, pharmacology, structural biology, and the multiplicity of endogenous GPCR ligands, in addition to a scarcity of biological and pharmacological tools for elucidating GPCR-mediated cellular processes beyond initial signaling events. Various mammalian, insect, and yeast cell models currently address some of these needs. Here, we review recent advances in yeast synthetic biology that are helping to catalyze new and unexpected conceptual and technical breakthroughs in GPCR-based medicine and biotechnology., Competing Interests: Declaration of Competing Interest D.G.I and N.J.K. declare no interests. G.J.T. was supported in part by an appointment to the NRC Research Associateship Program at the National Institute of Standards and Technology, administered by the Fellowships Office of the National Academies of Sciences, Engineering, and Medicine. Certain commercial equipment, instruments, or materials are identified to adequately specify the experimental procedure. Such identification implies neither recommendation or endorsement by the National Institute of Standards and Technology nor that the materials or equipment identified are necessarily the best available for the purpose. The views expressed in this publication are those of the authors and do not necessarily represent the views of the U.S. Department of Commerce or the National Institute of Standards and Technology., (Copyright © 2024 Elsevier Ltd. All rights reserved.)