期刊
CHEMICAL REVIEWS
卷 117, 期 1, 页码 67-110出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.chemrev.6b00056
关键词
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资金
- Biotechnology and Biosciences Research Council [BB/E019455/1, BB/L027887/1, BB/K019864/1]
- Danish Council for Strategic Research [11-116196]
- University of Southern Denmark
- Canadian Institutes of Health Research
- University of Glasgow
- Biotechnology and Biological Sciences Research Council [BB/E019455/1, BB/K019864/1, BB/L027887/1] Funding Source: researchfish
- BBSRC [BB/L027887/1, BB/K019864/1, BB/E019455/1] Funding Source: UKRI
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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