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anti-Human FFAR1 Antibodies:
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Mouse (Murine) Monoclonal FFAR1 Primary Antibody for FACS, IF - ABIN533478
Steneberg, Rubins, Bartoov-Shifman, Walker, Edlund: The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. in Cell metabolism 2005
Show all 5 Pubmed References
Human Polyclonal FFAR1 Primary Antibody for ELISA, WB - ABIN547449
Hardy, St-Onge, Joly, Langelier, Prentki: Oleate promotes the proliferation of breast cancer cells via the G protein-coupled receptor GPR40. in The Journal of biological chemistry 2005
Show all 2 Pubmed References
Cow (Bovine) Polyclonal FFAR1 Primary Antibody for WB - ABIN2792205
Sum, Tikhonova, Neumann, Engel, Raaka, Costanzi, Gershengorn: Identification of residues important for agonist recognition and activation in GPR40. in The Journal of biological chemistry 2007
Results indicate that FFAR4 plays a more critical role than FFAR1 in mediation of fat-regulated neurotensin release from neuroendocrine cells and in inhibitory crosstalk between MEK/ERK1/2 and AMPK in the control of NT release downstream of FFAR1 and FFAR4.
These results suggest that the cell motile and growth activities may be positively regulated through the induction of GPR40 by the long-term TAM treatment in MCF-7 cells.
Study conclude that free fatty acids are regulators of not only insulin but also glucagon and somatostatin secretion at fasting glucose concentrations from human islets and that FFAR1 is crucial in this effect. This implies that the effect of FFAR1 on hormone secretion is not restricted to amplification at elevated glucose concentrations, as previously reported, but rather fuel substrate dependent.
Study reports the 2.76-A crystal structure of human GPR40 complexed with compound 1 bound in a second structurally distinct allosteric site, located at the receptor side facing the membrane lipophilic environment. Binding of compound 1 stabilizes the intracellular loop 2 (ICL2) of GPR40 in a helical conformation. Mutagenesis studies in ICL2 shows that this loop is important for Gs alpha subunit coupling.
Data indicate that 20-HETE and FFAR1 function together in a positive feedback loop to enhance glucose-stimulated insulin secretion (GSIS).
Comparison with an additional 2.2-A structure of the human GPR40-MK-8666 binary complex reveals an induced-fit conformational coupling between the partial agonist and AgoPAM binding sites, involving rearrangements of the transmembrane helices 4 and 5 (TM4 and TM5) and transition of the intracellular loop 2 (ICL2) into a short helix.
Results show that GPR40 negatively regulated the cell motile and invasive activities of HT1080 cells suggesting that GPR40 negatively regulates the tumor progression of fibrosarcoma cells.
Brain free long-chain fatty acids-GPR40/FFA1 signaling might have an important role in the modulation of endogenous pain control systems. (review)
It regulates insulin secretion in pancreatic beta-cells. (review)
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.
GPR120 negatively and GPR40 positively regulate cellular functions during tumor progression in lung cancer cells.
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.
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.
Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4
results suggest that FFAR1 is the functionally dominant free fatty acid receptor in both human and guinea pig airway smooth muscle.
upregulation of GPR40 expression enhances the mitogenic response to epoxyeicosatrienoic acids
Palmitic acid boosted inflammatory response of microvascular endothelial cells to LPS via GPR40 and nSMase.
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
These results suggest that distinct effects of GPR120 and GPR40 are involved in the acquisition of malignant property in pancreatic cancer cells.
GPR40 functions via both G protein-mediated and beta-arrestin-mediated mechanisms; endogenous and synthetic ligands differentially engage these pathways to promote insulin secretion.
FFAR1 point mutation R258W abrogates fatty acid-induced insulin secretion
We found that FFAR1-/- female mice showed significant impairments in maternal behavior, and exhibited an emotionally altered behavior, when compared to WT mice. Our findings suggest that the dysfunction of brain PUFA-GPR40/FFAR1 signaling might induce damage to emotional and maternal behavior in female mice.
GPR120 suppresses adipose tissue lipolysis and synergizes with GPR40 in antidiabetic efficacy
GPR40 and (GPR120) act in concert in the hypothalamus to reduce energy efficiency and regulate the inflammation associated with obesity.
GPR40 role in the bone loss
These findings suggested that dysfunction of the GPR40/FFAR1 signaling pathway altered the endogenous pain control system and that this dysfunction might be associated with the development of chronic pain.
Together, our data indicate effects of AgoPAMs that go beyond glucose lowering previously observed with GPR40 partial agonist treatment with additional potential for weight loss.
These results support the hypothesis that mercaptoacetate stimulates food intake by blocking fatty acid effects on GPR40.
These results indicated that GPR120 enhanced and GPR40 inhibited the cell motile activity of highly migratory osteosarcoma cells.
Results suggest that brain GPR40/FFAR1 is associated with anxiety- and depression-related behavior regulated by the increment of noradrenaline in the brain.
Data revealed a weak influence of GPR40 agonist on osteoblast markers expression. Nevertheless, a significant increase in OPG expression was observed upon GW9508 treatment that contribute to explain the GPR40-related osteoporosis prevention
In the retinas of Vldlr(-/-) mice with low fatty acid uptake but high circulating lipid levels, we found that Ffar1 suppresses expression of the glucose transporter Glut1
activation of the hypothalamic GPR40/FFA1 signaling pathway may regulate beta-endorphin release via PC2, and regulate the endogenous pain control system
These results suggest that both PPARgamma and GRP40 are required for RSG-induced inhibition of mouse calvaria osteoblast differentiation, which is mediated through GSK3beta-dependent pathway.
GPR40 signaling pathway plays an important suppressive role in spinal nociceptive processing after inflammation or nerve injury
GPR 40/120 double-knockout mice are impaired in post-oral fat sensing.
GPR40/FFAR1 indirectly modulates organ-specific effects of CLAs.
This gene encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. The encoded protein is a receptor for medium and long chain free fatty acids and may be involved in the metabolic regulation of insulin secretion. Polymorphisms in this gene may be associated with type 2 diabetes.
free fatty acid receptor 1
, G protein-coupled receptor 40
, G-protein coupled receptor 40
, G protein-coupled receptor GPR40