-
Tytuł:
-
Chemogenetic Approaches to Explore the Functions of Free Fatty Acid Receptor 2.
-
Autorzy:
-
Milligan G; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, UK. Electronic address: .
Barki N; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, UK.
Tobin AB; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, UK. Electronic address: .
-
Źródło:
-
Trends in pharmacological sciences [Trends Pharmacol Sci] 2021 Mar; Vol. 42 (3), pp. 191-202. Date of Electronic Publication: 2021 Jan 22.
-
Typ publikacji:
-
Journal Article; Research Support, Non-U.S. Gov't; Review
-
Język:
-
English
-
Imprint Name(s):
-
Publication: Barking : Published By Elsevier In Association With The International Union Of Pharmacology
Original Publication: Amsterdam, Published by Elsevier in association with the International Union of Pharmacology.
-
MeSH Terms:
-
Receptors, Cell Surface*
Receptors, G-Protein-Coupled*
Animals ; Fatty Acids, Nonesterified ; Mice
-
Contributed Indexing:
-
Keywords: G protein-coupled receptor; designer receptor exclusively activated by designer drugs; short-chain fatty acid; transgenic mice
-
Substance Nomenclature:
-
0 (Fatty Acids, Nonesterified)
0 (Receptors, Cell Surface)
0 (Receptors, G-Protein-Coupled)
-
Entry Date(s):
-
Date Created: 20210126 Date Completed: 20210831 Latest Revision: 20210831
-
Update Code:
-
20240105
-
DOI:
-
10.1016/j.tips.2020.12.003
-
PMID:
-
33495026
-
Short-chain fatty acids are generated in large amounts by the intestinal microbiota. They activate both the closely related G protein-coupled receptors free fatty acid receptor 2 (FFA2) and free fatty acid receptor 3 (FFA3) that are considered therapeutic targets in diseases of immuno-metabolism. Limited and species-selective small-molecule pharmacology has restricted our understanding of the distinct roles of these receptors. Replacement of mouse FFA2 with a designer receptor exclusively activated by designer drug form of human FFA2 (hFFA2-DREADD) has allowed definition of specific roles of FFA2 in pharmacological and physiological studies conducted both ex vivo and in vivo, whilst overlay of murine disease models offers opportunities for therapeutic validation prior to human studies. Similar approaches can potentially be used to define roles of other poorly characterised receptors.
(Copyright © 2020 Elsevier Ltd. All rights reserved.)
