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Molecular Pharmacology

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The Pharmacology and Function of Receptors for Short-Chain Fatty Acids

Daniele Bolognini, Andrew B. Tobin, Graeme Milligan and Catherine E. Moss
Molecular Pharmacology March 2016, 89 (3) 388-398; DOI: https://doi.org/10.1124/mol.115.102301
Daniele Bolognini
Molecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, University of Glasgow, Glasgow, Scotland, United Kingdom (D.B., G.M.); and Medical Research Council Toxicology Unit, University of Leicester, Leicester, United Kingdom (A.B.T., C.E.M.)
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Andrew B. Tobin
Molecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, University of Glasgow, Glasgow, Scotland, United Kingdom (D.B., G.M.); and Medical Research Council Toxicology Unit, University of Leicester, Leicester, United Kingdom (A.B.T., C.E.M.)
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Graeme Milligan
Molecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, University of Glasgow, Glasgow, Scotland, United Kingdom (D.B., G.M.); and Medical Research Council Toxicology Unit, University of Leicester, Leicester, United Kingdom (A.B.T., C.E.M.)
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Catherine E. Moss
Molecular Pharmacology Group, Institute of Molecular, Cell and Systems Biology, University of Glasgow, Glasgow, Scotland, United Kingdom (D.B., G.M.); and Medical Research Council Toxicology Unit, University of Leicester, Leicester, United Kingdom (A.B.T., C.E.M.)
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Abstract

Despite some blockbuster G protein–coupled receptor (GPCR) drugs, only a small fraction (∼15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry. One way that this issue might be addressed is via translation of recent deorphanization programs that have opened the prospect of extending the reach of new medicine design to novel receptor types with potential therapeutic value. Prominent among these receptors are those that respond to short-chain free fatty acids of carbon chain length 2–6. These receptors, FFA2 (GPR43) and FFA3 (GPR41), are each predominantly activated by the short-chain fatty acids acetate, propionate, and butyrate, ligands that originate largely as fermentation by-products of anaerobic bacteria in the gut. However, the presence of FFA2 and FFA3 on pancreatic β-cells, FFA3 on neurons, and FFA2 on leukocytes and adipocytes means that the biologic role of these receptors likely extends beyond the widely accepted role of regulating peptide hormone release from enteroendocrine cells in the gut. Here, we review the physiologic roles of FFA2 and FFA3, the recent development and use of receptor-selective pharmacological tool compounds and genetic models available to study these receptors, and present evidence of the potential therapeutic value of targeting this emerging receptor pair.

Footnotes

    • Received November 2, 2015.
    • Accepted December 29, 2015.
  • D.B. and C.E.M. contributed equally to this work.

  • These studies were funded in part by the Biotechnology and Biosciences Research Council [Grants BB/K019864/1 and BB/K019856/1].

  • dx.doi.org/10.1124/mol.115.102301.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 89 (3)
Molecular Pharmacology
Vol. 89, Issue 3
1 Mar 2016
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Rapid CommunicationMinireview

Pharmacology of Short-Chain Fatty Acid Receptors

Daniele Bolognini, Andrew B. Tobin, Graeme Milligan and Catherine E. Moss
Molecular Pharmacology March 1, 2016, 89 (3) 388-398; DOI: https://doi.org/10.1124/mol.115.102301

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Rapid CommunicationMinireview

Pharmacology of Short-Chain Fatty Acid Receptors

Daniele Bolognini, Andrew B. Tobin, Graeme Milligan and Catherine E. Moss
Molecular Pharmacology March 1, 2016, 89 (3) 388-398; DOI: https://doi.org/10.1124/mol.115.102301
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  • Article
    • Abstract
    • Introduction
    • FFA2/FFA3 Receptor Structure and Signal Transduction
    • Physiologic Roles of FFA2/FFA3
    • Experimental Challenges and Current Perspectives for the Validation of FFA2/FFA3 as Therapeutic Target(s)
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