A kinetic view of GPCR allostery and biased agonism

Lane, J. Robert; May, Lauren T.; Parton, Robert G.; Sexton, Patrick M.; Christopoulos, Arthur

doi:10.1038/nchembio.2431

All Outputs (3)

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.

Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites (2018)
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The D1 dopamine receptor is linked to a variety of neuropsychiatric disorders and represents an attractive drug target for the enhancement of cognition in schizophrenia, Alzheimer disease, and other disorders. Positive allosteric modulators (PAMs), w... Read More about Identification of Positive Allosteric Modulators of the D1 Dopamine Receptor That Act at Diverse Binding Sites.

A kinetic view of GPCR allostery and biased agonism (2017)
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