Property Summary

NCBI Gene PubMed Count 57
Grant Count 23
R01 Count 3
Funding $1,565,793.13
PubMed Score 262.35
PubTator Score 154.61

Knowledge Summary

Patent (29,866)

TINX Plot

  Disease Relevance (3)

Expression

Gene RIF (48)

PMID Text
26974599 Data from molecular docking simulations suggest that the binding pocket of GPR40 exhibits binding of free fatty acids (FFA) with chain lengths of C15 or fewer; for FFA with lengths longer than C15, part of alkyl chain extends out of binding pocket.
26968637 GPR120 negatively and GPR40 positively regulate cellular functions during tumor progression in lung cancer cells.
26869446 Increased membrane permeability induced by linoleic acid is mediated by an intracellular signaling pathway activated by GPR40 that leads to an increase in membrane levels of Cx43 phosphorylated at serine 373 via Akt.
26505901 These data demonstrate that R104 in GPR40 is critically involved in the normal receptor functions. Interestingly, R104P is a registered single-nucleotide polymorphism of GPR40.
26408932 knocking down the expression of the regulatory subunit PKAR1alpha, thereby reproducing the effects of IL-1beta and PGE on VSMCs, we demonstrated the contribution of PKA activity to the observed behavior of VSMCs
26342087 results suggest that FFAR1 is the functionally dominant free fatty acid receptor in both human and guinea pig airway smooth muscle.
26282200 These results suggest that distinct effects of GPR120 and GPR40 are involved in the acquisition of malignant property in pancreatic cancer cells.
26157145 GPR40 functions via both G protein-mediated and beta-arrestin-mediated mechanisms; endogenous and synthetic ligands differentially engage these pathways to promote insulin secretion.
26105050 GPR40 and PPARgamma can function as an integrated two-receptor signal transduction pathway, a finding with implications for rational antidiabetic drug development.
26028412 It regulates insulin secretion in pancreatic beta-cells. (review)
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AA Sequence

MDLPPQLSFGLYVAAFALGFPLNVLAIRGATAHARLRLTPSLVYALNLGCSDLLLTVSLPLKAVEALASG      1 - 70
AWPLPASLCPVFAVAHFFPLYAGGGFLAALSAGRYLGAAFPLGYQAFRRPCYSWGVCAAIWALVLCHLGL     71 - 140
VFGLEAPGGWLDHSNTSLGINTPVNGSPVCLEAWDPASAGPARFSLSLLLFFLPLAITAFCYVGCLRALA    141 - 210
RSGLTHRRKLRAAWVAGGALLTLLLCVGPYNASNVASFLYPNLGGSWRKLGLITGAWSVVLNPLVTGYLG    211 - 280
RGPGLKTVCAARTQGGKSQK                                                      281 - 300
//

Text Mined References (57)

PMID Year Title
26974599 2016 Investigation of the Binding Interaction of Fatty Acids with Human G Protein-Coupled Receptor 40 Using a Site-Specific Fluorescence Probe by Flow Cytometry.
26968637 2016 Diverse effects of G-protein-coupled free fatty acid receptors on the regulation of cellular functions in lung cancer cells.
26869446 2016 Linoleic acid permeabilizes gastric epithelial cells by increasing connexin 43 levels in the cell membrane via a GPR40- and Akt-dependent mechanism.
26505901 2015 A Single Amino Acid Mutation (R104P) in the E/DRY Motif of GPR40 Impairs Receptor Function.
26408932 2015 Free fatty acid receptor 1 (FFAR1/GPR40) signaling affects insulin secretion by enhancing mitochondrial respiration during palmitate exposure.
26342087 2015 Novel identification of the free fatty acid receptor FFAR1 that promotes contraction in airway smooth muscle.
26282200 2015 Different roles of GPR120 and GPR40 in the acquisition of malignant properties in pancreatic cancer cells.
26157145 2015 ?-Arrestin Recruitment and Biased Agonism at Free Fatty Acid Receptor 1.
26105050 2015 G Protein-coupled Receptor 40 (GPR40) and Peroxisome Proliferator-activated Receptor ? (PPAR?): AN INTEGRATED TWO-RECEPTOR SIGNALING PATHWAY.
26028412 2015 [Free Fatty Acid Receptor Family: A New Therapeutic Target for Metabolic Diseases].
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