Article Figures & Data
Figures
- Fig. 1.
Human FFA1 receptor. Snake plot of human FFA1 receptor (NP005924). TM helices were assigned according to the PHD algorithm (Rost, 1996). Conserved motifs common to class A GPCRs are shown in dark gray (white lettering) as are the two known human polymorphisms, Arg211His (Hamid et al., 2005; Ogawa et al., 2005) and Asp175Asn (Hamid et al., 2005). The FFA1 receptor has two putative N-glycosylation sites (Asn155 and Asn165; motif: Asn-x-Ser/Thr) and two potential protein kinase C phosphorylation sites (Thr215 and Ser298, Ser/Thr-x-Arg/Lys). Basic residues conserved across the FFA receptor family and those additionally implicated in receptor activation by Tikhonova et al. (2007) are indicated in black (white lettering).
- Fig. 2.
Amino acid sequence alignment of FFA1, FFA2, and FFA3. Amino acid sequences corresponding to human FFA1, FFA2, and FFA3 were aligned using the ClustalW2 algorithm. Transmembrane regions are boxed with a dashed line. Residues implicated in the ligand binding site of the FFA1 and the corresponding residues in FFA2 and FFA3 are boxed with a continuous line. Accession numbers are as follows: human FFA1, NP005294; human FFA2, NP005297; and human FFA3, NP005295.
Tables
Receptor Name Human Free Fatty Acid Receptors FFA1 FFA2 FFA3 Previous names GPR40, FFAR1 GPR43, FFAR2 GPR41, FFAR3 Gene location 19q13.1 19q13.1 19q13.1 Amino acid length 300 330 346 % amino acid identity 33% to FFA2 33% to FFA1 34% to FFA1 34% to FFA3 43% to FFA3 43% to FFA2 Activating fatty acid (carbon chain length) C6–C22, saturated and unsaturated C1–C6 C1–C6 Synthetic agonists (commercially available) Rosiglitazone; troglitazone; GW9508X G protein coupling Gαq/11 and Gαi/o Gαi/o and Gαq/11 Gαi/o Human tissue distribution Highest expression in pancreatic islets, also in gastrointestinal tract, brain, and monocytes Immune cells including peripheral blood leukocytes, neutrophils, eosinophils; adipocytes; distal ileum; colon Adipose tissue; spleen; lymph node; bone marrow; peripheral blood mononuclear cells Tissue function Potentiation of GSIS in pancreatic islets; increase in glucagon secretion Stimulation of adipogenesis; inhibition of lipolysis; activation of polymorphonuclear cells Increase in leptin production Disease Type 2 diabetes Knockout animal Yes Yes No Phenotype of knockout Reduction in capacity of FFAs to augment GSIS Loss of acetate-mediated reduction in plasma FFA levels
In this issue
Jump to section
- Article
- Abstract
- I. Introduction
- II. Cloning of cDNA for Free Fatty Acid Receptors 1, 2, and 3
- III. Free Fatty Acid Receptor Structure
- IV. Deorphanization of Free Fatty Acid Receptors and Modes of Signal Transduction
- V. Tissue Distribution of Free Fatty Acid Receptors
- VI. Free Fatty Acid Receptor 1 Synthetic Agonists and Antagonists
- VII. Molecular Basis of Free Fatty Acid Receptor 1 Activation
- VIII. Physiological Roles of Free Fatty Acid Receptors
- IX. Conclusions
- Acknowledgments
- Footnotes
- References
- Figures & Data
- Info & Metrics
- eLetters