Free fatty acid receptor 2

FFAR2

Identifiers

FFAR2, FFA2R, GPR43, free fatty acid receptor 2

External IDs

MGI: 2441731 HomoloGene: 133911 GeneCards: FFAR2

Targeted by Drug

butyric acid, isobutyric acid, (E)-2,3-dimethylacrylic acid, valeric acid, propionic acid^[1]

Gene ontology
Molecular function	• G-protein coupled receptor activity • signal transducer activity • protein binding • lipid binding
Cellular component	• integral component of membrane • cell projection • membrane • plasma membrane • integral component of plasma membrane
Biological process	• mucosal immune response • G-protein coupled receptor signaling pathway • glucose homeostasis • immune system process • positive regulation of cytokine production involved in immune response • leukocyte chemotaxis involved in inflammatory response • lipid storage • cellular response to fatty acid • positive regulation of acute inflammatory response to non-antigenic stimulus • cell surface pattern recognition receptor signaling pathway • positive regulation of chemokine production • positive regulation of interleukin-8 secretion • inflammatory response • regulation of peptide hormone secretion • fat cell differentiation • regulation of acute inflammatory response • signal transduction
Sources:Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

Entrez


2867


233079

Ensembl


ENSG00000126262


ENSMUSG00000051314

UniProt


O15552


Q8VCK6

RefSeq (mRNA)


NM_005306


NM_001168509 NM_001168510 NM_001168511 NM_001168512 NM_146187

RefSeq (protein)


NP_005297.1


NP_001161981.1 NP_001161982.1 NP_001161983.1 NP_001161984.1 NP_666299.1

Location (UCSC)

Chr 19: 35.44 – 35.45 Mb

Chr 7: 30.82 – 30.82 Mb

PubMed search

^[2]

^[3]

Wikidata

View/Edit Human

View/Edit Mouse

Free fatty acid receptor 2 (FFA2) is a G-protein coupled receptor encoded by the FFAR2 gene.^[4]

Expression

FFAR2 mRNA is expressed in adipose tissue, pancreas, spleen, lymph nodes, bone marrow, and peripheral blood mononuclear cells.^[5]^[6] FFAR2 transcription is regulated by the XBP1 transcription factor which binds to the core promoter.^[7]

Function

Mouse studies utilizing Ffar2 gene deletions have implicated the receptor in the regulation of energy metabolism and immune responses.^[8] However, discrepancies between the pathways activated by FFAR2 agonists in human cells and the equivalent murine counterparts have been observed.^[9]^[10]^[11]

References

↑ "Drugs that physically interact with Free fatty acid receptor 2 view/edit references on wikidata".
↑ "Human PubMed Reference:".
↑ "Mouse PubMed Reference:".
↑ "Entrez Gene: FFAR2 free fatty acid receptor 2".
↑ Nilsson NE, Kotarsky K, Owman C, Olde B (2003). "Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids.". Biochem. Biophys. Res. Commun. 303 (4): 1047–52. doi:10.1016/S0006-291X(03)00488-1. PMID 12684041.
↑ Le Poul E, Loison C, Struyf S (2003). "Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.". J. Biol. Chem. 278 (28): 25481–9. doi:10.1074/jbc.M301403200. PMID 12711604.
↑ Ang Z, Er JZ, Ding JL (2015). "The short-chain fatty acid receptor GPR43 is transcriptionally regulated by XBP1 in human monocytes.". Sci Rep. 5: 8134. doi:10.1038/srep08134. PMID 25633224.
↑ Bindels, Laure B.; Dewulf, Evelyne M.; Delzenne, Nathalie M. (2013-04-01). "GPR43/FFA2: physiopathological relevance and therapeutic prospects". Trends in Pharmacological Sciences. 34 (4): 226–232. doi:10.1016/j.tips.2013.02.002. ISSN 1873-3735. PMID 23489932.
↑ Dewulf, Evelyne M.; Ge, Qian; Bindels, Laure B.; Sohet, Florence M.; Cani, Patrice D.; Brichard, Sonia M.; Delzenne, Nathalie M. (2013-01-17). "Evaluation of the relationship between GPR43 and adiposity in human". Nutrition & Metabolism. 10 (1): 11. doi:10.1186/1743-7075-10-11. PMC 3577645. PMID 23327542.
↑ Priyadarshini, Medha; Villa, Stephanie R.; Fuller, Miles; Wicksteed, Barton; Mackay, Charles R.; Alquier, Thierry; Poitout, Vincent; Mancebo, Helena; Mirmira, Raghavendra G. (2015-07-01). "An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion". Molecular Endocrinology (Baltimore, Md.). 29 (7): 1055–1066. doi:10.1210/me.2015-1007. ISSN 1944-9917. PMC 4484778. PMID 26075576.
↑ Ang, Zhiwei; Er, Jun Zhi; Tan, Nguan Soon; Lu, Jinhua; Liou, Yih-Cherng; Grosse, Johannes; Ding, Jeak Ling (2016-09-26). "Human and mouse monocytes display distinct signalling and cytokine profiles upon stimulation with FFAR2/FFAR3 short-chain fatty acid receptor agonists". Scientific Reports. 6: 34145. doi:10.1038/srep34145. ISSN 2045-2322. PMC 5036191. PMID 27667443.

External links

"Free Fatty Acid Receptors: FFA2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

Brown AJ, Jupe S, Briscoe CP (2005). "A family of fatty acid binding receptors.". DNA Cell Biol. 24 (1): 54–61. doi:10.1089/dna.2005.24.54. PMID 15684720.
Sawzdargo M, George SR, Nguyen T, et al. (1997). "A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1.". Biochem. Biophys. Res. Commun. 239 (2): 543–7. doi:10.1006/bbrc.1997.7513. PMID 9344866.
Senga T, Iwamoto S, Yoshida T, et al. (2003). "LSSIG is a novel murine leukocyte-specific GPCR that is induced by the activation of STAT3.". Blood. 101 (3): 1185–7. doi:10.1182/blood-2002-06-1881. PMID 12393494.
Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
Brown AJ, Goldsworthy SM, Barnes AA, et al. (2003). "The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.". J. Biol. Chem. 278 (13): 11312–9. doi:10.1074/jbc.M211609200. PMID 12496283.
Nilsson NE, Kotarsky K, Owman C, Olde B (2003). "Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids.". Biochem. Biophys. Res. Commun. 303 (4): 1047–52. doi:10.1016/S0006-291X(03)00488-1. PMID 12684041.
Le Poul E, Loison C, Struyf S, et al. (2003). "Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.". J. Biol. Chem. 278 (28): 25481–9. doi:10.1074/jbc.M301403200. PMID 12711604.
Grimwood J, Gordon LA, Olsen A, et al. (2004). "The DNA sequence and biology of human chromosome 19.". Nature. 428 (6982): 529–35. doi:10.1038/nature02399. PMID 15057824.
Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928. PMID 15489334.
Yonezawa T, Kobayashi Y, Obara Y (2007). "Short-chain fatty acids induce acute phosphorylation of the p38 mitogen-activated protein kinase/heat shock protein 27 pathway via GPR43 in the MCF-7 human breast cancer cell line.". Cell. Signal. 19 (1): 185–93. doi:10.1016/j.cellsig.2006.06.004. PMID 16887331.

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3

Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)

Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)

Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine (D1 D2 D3 D4 D5) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 (1 2) FPRL1 OXE Prostaglandin (DP (1 2), EP (1 2 3 4), FP) Prostacyclin Thromboxane

Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide	B/W (1 2) FF (1 2) S Y (1 2 4 5) Neuromedin (B U (1 2)) Neurotensin (1 2)

Other	Anaphylatoxin (C3a C5a) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor Gonadotropin-releasing hormone (1 2) Ghrelin Kisspeptin Luteinizing hormone/choriogonadotropin MAS (1 1L D E F G X1 X2 X3 X4) Melanocortin (1 2 3 4 5) MCHR (1 2) Motilin Opioid (Delta Kappa Mu Nociceptin & Zeta, but not Sigma) Orexin (1 2) Oxytocin Prokineticin (1 2) Prolactin-releasing peptide Relaxin (1 2 3 4) Somatostatin (1 2 3 4 5) Tachykinin (1 2 3) Thyrotropin Thyrotropin-releasing hormone Urotensin-II Vasopressin (1A 1B 2)

Miscellaneous

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)

Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin like

Adhesion	ADGRG (1 2 3 4 5 6 7)

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste	TAS1R (1 2 3) TAS2R (1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor)

Other	Calcium-sensing receptor GABA B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled / Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)

Smoothened	Smoothened

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Free fatty acid receptor 2

Expression

Function

See also

References

External links

Further reading