The DOI matches its Crossref record; 29 of the 29 references it cites were found in a registry or an index.
Complex Pharmacology of Free Fatty Acid Receptors
Open accessAbstract
G protein-coupled receptors (GPCRs) are historically the most successful family of drug targets. In recent times it has become clear that the pharmacology of these receptors is far more complex than previously imagined. Understanding of the pharmacological regulation of GPCRs now extends beyond simple competitive agonism or antagonism by ligands interacting with the orthosteric binding site of the receptor to incorporate concepts of allosteric agonism, allosteric modulation, signaling bias, constitutive activity, and inverse agonism. Herein, we consider how evolving concepts of GPCR pharmacology have shaped understanding of the complex pharmacology of receptors that recognize and are activated by nonesterified or "free" fatty acids (FFAs). The FFA family of receptors is a recently deorphanized set of GPCRs, the members of which are now receiving substantial interest as novel targets for the treatment of metabolic and inflammatory diseases. Further understanding of the complex pharmacology of these receptors will be critical to unlocking their ultimate therapeutic potential.
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Cites
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Cited by
Free Fatty Acid Receptors in Health and Disease
Kimura, I., Ichimura, A., Ohue-Kitano, R., & Igarashi, M. (2020) · Physiological Reviews · doi:10.1152/physrev.00041.2018 · Cited by 1,018
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Effect of probiotics on depressive symptoms: a meta-analysis of human studies
Goh, K. K., Liu, Y.-W., Kuo, P.-H., Chung, Y.-C. E., Lu, M.-L., & Chen, C.-H. (2019) · Psychiatry Research · doi:10.1016/j.psychres.2019.112568 · Cited by 123
G Protein–Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus
Riddy, D. M., Delerive, P., Summers, R. J., Sexton, P. M., & Langmead, C. J. (2018) · Pharmacological Reviews · doi:10.1124/pr.117.014373 · Cited by 108
Metadata
- Authors
- Milligan, G., Shimpukade, B., Ulven, T., & Hudson, B. D.
- Venue
- Chemical Reviews
- Publisher
- American Chemical Society (ACS)
- Published
- 2016-06-14
- Volume
- 117
- Issue
- 1
- Pages
- 67-110
- ISSN
- 0009-2665 (ISSN-L)
- 1520-6890
- OpenAlex
- W2429754450
- Cited by
- 267
- References
- 29
- FWCI
- 1.69
- Type
- journal article
- Language
- en
- Open access
- hybrid
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