Low intrinsic efficacy for G protein activation can explain the improved side-effect profile of new opioid agonists

Gillis, Alexander; Gondin, Arisbel B.; Kliewer, Andrea; Sanchez, Julie; Lim, Herman D.; Alamein, Claudia; Manandhar, Pradeep; Santiago, Marina; Fritzwanker, Sebastian; Schmidel, Frank; Katte, Timothy A.; Reekie, Tristan; Grimsey, Natasha L.; Kassiou, Michael; Kellam, Barrie; Krasel, Cornelius; Halls, Michelle L.; Connor, Mark; Lane, J. Robert; Schulz, Stefan; Christie, Macdonald J.; Canals, Meritxell

doi:10.1126/scisignal.aaz3140

All Outputs (5)

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Low intrinsic efficacy for G protein activation can explain the improved side-effect profile of new opioid agonists (2020)
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Biased agonism at G protein–coupled receptors describes the phenomenon whereby some drugs can activate some downstream signaling activities to the relative exclusion of others. Descriptions of biased agonism focusing on the differential engagement of... Read More about Low intrinsic efficacy for G protein activation can explain the improved side-effect profile of new opioid agonists.