Abstract
Yeast assays for G-protein-coupled receptors have many attractions due to their simplicity, low cost, and lack of endogenous receptors. Since the first report of functional coupling of the human beta 2 adrenergic receptor to the yeast pheromone-response pathway in 1990, the technology has developed to a point at which more than 30 heterologous GPCRs are now published to couple. Major breakthroughs have come from an understanding of receptor-G protein interactions, alongside advances in knowledge of the structure of heterotrimeric G proteins. Yeast screens have been used to identify ligands both from compound collections and through the autocrine expression of peptide libraries. Yeast genetics has also been applied to a functional analysis of GPCRs and peptide ligands. In this review we describe the historical development of yeast GPCR assay systems and their current applications.
MeSH terms
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Biochemistry / methods*
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Biotechnology / methods
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GTP-Binding Protein alpha Subunits*
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GTP-Binding Protein alpha Subunits, Gq-G11
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GTP-Binding Protein beta Subunits*
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GTP-Binding Protein gamma Subunits*
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GTP-Binding Proteins / chemistry
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GTP-Binding Proteins / metabolism*
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Heterotrimeric GTP-Binding Proteins / chemistry
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Humans
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Ligands
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Melatonin / pharmacology
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Models, Biological
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Models, Molecular
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Peptides / chemistry
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Pheromones / metabolism
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Protein Binding
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Protein Conformation
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Receptors, Cell Surface / chemistry
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Receptors, Cell Surface / metabolism*
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Receptors, Cytoplasmic and Nuclear / chemistry
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Receptors, Melatonin
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Saccharomyces cerevisiae / metabolism*
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Saccharomyces cerevisiae Proteins / chemistry
Substances
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GTP-Binding Protein alpha Subunits
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GTP-Binding Protein beta Subunits
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GTP-Binding Protein gamma Subunits
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Ligands
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Peptides
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Pheromones
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Receptors, Cell Surface
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Receptors, Cytoplasmic and Nuclear
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Receptors, Melatonin
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STE18 protein, S cerevisiae
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Saccharomyces cerevisiae Proteins
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Ste4 protein, S cerevisiae
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GTP-Binding Proteins
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GPA1 protein, S cerevisiae
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GTP-Binding Protein alpha Subunits, Gq-G11
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Heterotrimeric GTP-Binding Proteins
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Melatonin