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Broichhagen, Johannes; Johnston, Natalie R.; Ohlen, Yorrick von; Meyer-Berg, Helena; Jones, Ben J.; Bloom, Stephen R.; Rutter, Guy A.; Trauner, Dirk; Hodson, David J. (2016): Allosteric Optical Control of a Class B G-Protein-Coupled Receptor. In: Angewandte Chemie-international Edition, Vol. 55, No. 19: pp. 5865-5868
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Allosteric regulation promises to open up new therapeutic avenues by increasing drug specificity at G-protein-coupled receptors (GPCRs). However, drug discovery efforts are at present hampered by an inability to precisely control the allosteric site. Herein, we describe the design, synthesis, and testing of PhotoETP, a light-activated positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), a classB GPCR involved in the maintenance of glucose homeostasis in humans. PhotoETP potentiates Ca2+, cAMP, and insulin responses to glucagon-like peptide-1 and its metabolites following illumination of cells with blue light. PhotoETP thus provides a blueprint for the production of small-molecule classB GPCR allosteric photoswitches, and may represent a useful tool for understanding positive cooperativity at the GLP-1R.