Functional Selectivity and Biased Receptor Signaling
The Journal of Pharmacology and Experimental Therapeutics, ISSN: 0022-3565, Vol: 336, Issue: 2, Page: 296-302
2011
- 424Citations
- 379Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations424
- Citation Indexes424
- 424
- CrossRef415
- Captures379
- Readers379
- 379
Article Description
With the emergence of information describing functional selectivity and biased agonists and antagonists has come a lack of confidence in “one size fits all” assays for detection of agonism. Seven-transmembrane receptors are pleiotropic with respect to the signaling protein to which they couple in a cell, and many conformations of the receptor can be formed; this leads to systems where ligands can stabilize unique conformations that go on to selectively activate signaling pathways. Thus, such “biased” ligands can produce cell-specific agonism that may require targeted assays to detect and quantify. It also predicts that ligands can have many different efficacies for the many behaviors that the receptor can exhibit (referred to as “pluridimensional efficacy”), leading to a breakdown in the common classifications of agonist and antagonist. This all poses unique challenges to the pharmacologic nomenclature of drugs, the detection and optimization of new drugs, and the association of phenotypic clinical profiles with pharmacological properties of drugs.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0022356524462058; http://dx.doi.org/10.1124/jpet.110.173948; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=78751498756&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/21030484; https://linkinghub.elsevier.com/retrieve/pii/S0022356524462058; https://dx.doi.org/10.1124/jpet.110.173948; http://jpet.aspetjournals.org/content/336/2/296
Elsevier BV
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