The DOI matches its Crossref record; 100 of the 100 references it cites were found in a registry or an index.
Inverse, protean, and ligand‐selective agonism: matters of receptor conformation
Abstract
Concepts regarding the mechanisms by which drugs activate receptors to produce physiological response have progressed beyond considering the re¬ceptor as a simple on‐off switch. Current evidence suggests that the idea that agonists produce only vary¬ing degrees of receptor activation is obsolete and must be reconciled with data to show that agonist efficacy has texture as well as magnitude. Thus, agonists can block system constitutive response (inverse agonists), behave as positive and inverse agonists on the same receptor (protean agonists), and differ in the stimulus pattern they produce in physiological systems (ligand‐selective agonists). The molecular mechanism for this seemingly diverse array of activities is the same, namely, the selective microaffinity of ligands for different conformational states of the receptor. This paper reviews evidence for the existence of the various types of agonism and the potential therapeutic utility of differ¬ent agonist types.—Kenakin, T. Inverse, protean, and ligand‐selective agonism: matters of receptor confor¬mation. FASEB J. 15, 598‐611 (2001)
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Nichols, D. E., & Nichols, C. D. (2008) · Chemical Reviews · doi:10.1021/cr078224o · Cited by 895
GRKs and β-arrestins: roles in receptor silencing, trafficking and signaling
Reiter, E., & Lefkowitz, R. J. (2006) · Trends in Endocrinology & Metabolism · doi:10.1016/j.tem.2006.03.008 · Cited by 666
Cannabinoid Receptors: Where They are and What They do
Mackie, K. (2008) · Journal of Neuroendocrinology · doi:10.1111/j.1365-2826.2008.01671.x · Cited by 638
G protein coupled receptor structure and activation
Kobilka, B. K. (2007) · Biochimica et Biophysica Acta (BBA) - Biomembranes · doi:10.1016/j.bbamem.2006.10.021 · Cited by 623
High-throughput screening assays for the identification of chemical probes
Inglese, J., Johnson, R. L., Simeonov, A., Xia, M., Zheng, W., Austin, C. P., & Auld, D. S. (2007) · Nature Chemical Biology · doi:10.1038/nchembio.2007.17 · Cited by 614
Metadata
- Authors
- KENAKIN, T.
- Venue
- The FASEB Journal
- Publisher
- Wiley
- Published
- 2001-03
- Volume
- 15
- Issue
- 3
- Pages
- 598-611
- ISSN
- 0892-6638 (ISSN-L)
- 1530-6860
- OpenAlex
- W2087135060
- Cited by
- 408
- References
- 100
- FWCI
- 8.90
- Type
- journal article
- Language
- en
- Open access
- closed
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