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G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases (2019)
Journal Article
Canals, M., Poole, D. P., Veldhuis, N. A., Schmidt, B. L., Bunnett, N. W., & Bunnett, N. (2019). G protein-coupled receptors are dynamic regulators of digestion and targets for digestive diseases. Gastroenterology, doi:10.1053/j.gastro.2019.01.266

G protein-coupled receptors (GPCRs) are the largest family of transmembrane signaling proteins. Within the gastrointestinal tract, GPCRs expressed by epithelial cells sense contents of the lumen, and GPCRs expressed by epithelial cells, myocytes, neu... Read More

Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer (2019)
Journal Article
Blasco-Benito, S., Moreno, E., Seijo-Vila, M., Tundidor, I., Andradas, C., Caffarel, M. M., …Sánchez, C. (2019). Therapeutic targeting of HER2–CB2R heteromers in HER2-positive breast cancer. Proceedings of the National Academy of Sciences, 1-10. doi:10.1073/pnas.1815034116

Although human epidermal growth factor receptor 2 (HER2)-targeted therapies have dramatically improved the clinical outcome of HER2-positive breast cancer patients, innate and acquired resistance remains an important clinical challenge. New therapeut... Read More

Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations (2018)
Journal Article
Civciristov, S., Ellisdon, A. M., Suderman, R., Pon, C. K., Evans, B. A., Kleifeld, O., …Halls, M. L. (2018). Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations. Science Signaling, 11(551), doi:10.1126/scisignal.aan1188

G protein–coupled receptors (GPCRs) are the largest class of cell surface signaling proteins, participate in nearly all physiological processes, and are the targets of 30% of marketed drugs. Typically, nanomolar to micromolar concentrations of ligand... Read More

Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor (2014)
Journal Article
Abdul-Ridha, A., López, L., Keov, P., Thal, D. M., Mistry, S. N., Sexton, P. M., …Christopoulos, A. (2014). Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor. Journal of Biological Chemistry, 289(9), 6067-6079. doi:10.1074/jbc.M113.539080

Benzylquinolone carboxylic acid (BQCA) is an unprecedented example of a selective positive allosteric modulator of acetylcholine at the M1 muscarinic acetylcholine receptor (mAChR). To probe the structural basis underlying its selectivity, we utilize... Read More