Distribution and regulation of protein expression of the free fatty acid receptor GPR120

Miyauchi, Satoshi; Hirasawa, Akira; Iga, Tomoyo; Liu, Ning; Itsubo, Chisato; Sadakane, Keiko; Hara, Takafumi; Tsujimoto, Gozoh

doi:10.1007/s00210-008-0390-8

Cited by 136 publications

(98 citation statements)

References 13 publications

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“…Of note, with the possible exception of the third proposed option, all of these criteria may also be applied to antibodies raised against targets other than GPCR. A recent report demonstrates an additional approach based on tagged receptors, in which a GPCR antibody detects the same protein as the antibody against the tag (Miyauchi et al 2009); however, this approach needs to be validated in further studies using the hard criteria described above.…”

Section: Criteria To Demonstrate Receptor Antibody Specificitymentioning

confidence: 99%

How reliable are G-protein-coupled receptor antibodies?

Michel

Wieland

Tsujimoto

2009

Naunyn-Schmied Arch Pharmacol

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281

204

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A cluster of manuscripts in this issue of the Journal highlights a lack of selectivity of 49 antibodies against 19 subtypes of α 1 -and β-adrenoceptors, muscarinic, dopamine and galanin receptors as well as vanilloid (TRPV1) receptors. Taken together these data demonstrate that lack of selectivity appears to be the rule rather than the exception for antibodies against G-protein-coupled and perhaps also other receptors. Thus, the previously often applied validation of such antibodies by the disappearance of staining in the presence of blocking peptide, i.e. the antigen against which the antibody was raised, alone is insufficient to demonstrate specificity. We propose that receptor antibodies should be validated by at least one of the following techniques: a) disappearance of staining in knock-out animals of the target receptor, b) reduction of staining upon knock-down approaches such as siRNA treatment, c) selectivity of staining in immunoblots or immunocytochemistry for the target receptor vs. related subtypes when expressed in the same cell line and/or d) antibodies raised against multiple distinct epitopes of a receptor yielding very similar staining patterns. Other issues of consideration to obtain reliable results based on receptor antibodies in applications such as immunohistochemistry or immunoblotting are also being discussed.

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Section: Criteria To Demonstrate Receptor Antibody Specificitymentioning

confidence: 99%

How reliable are G-protein-coupled receptor antibodies?

Michel

Wieland

Tsujimoto

2009

Naunyn-Schmied Arch Pharmacol

Self Cite

281

204

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“…Furthermore, it is also evident that any effects of orally administered GPR120 agonists on insulin secretion are likely to be mediated mainly by indirect actions on the intestine. This is because GPR120 is expressed on intestinal enteroendocrine cells where it regulates the secretion of incretins such as GIP, GLP-1 and cholecystokinin [130][131][132][133][134]. Therefore, on the basis of these considerations, it seems unlikely that GPR120 plays any direct role in regulating insulin secretion.…”

Section: Gpr120mentioning

confidence: 99%

G-protein coupled receptors mediating long chain fatty acid signalling in the pancreatic beta-cell

Morgan¹,

Dhayal²

2009

Biochemical Pharmacology

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It is increasingly clear that some of the effects of both free and derivatised long chain fatty acids in pancreatic beta-cells are mediated by a group of G-protein coupled receptors. Some of these display close structural homology while others are more divergent. This Commentary reviews the expression and functional roles of three such molecules, GPR40, GPR119 and GPR120. GPR40 is the best characterised of this group and appears to mediate the acute stimulatory effects of long chain fatty acids on insulin secretion. GPR40 has also been proposed as a potential mediator of fatty acid toxicity but this is more controversial. GPR119 is also involved in stimulation of insulin secretion and responds primarily to ethanolamine derivatives of long chain fatty acids and also to some lysophospholipids rather than to free fatty acids. It may represent a useful target for the development of new insulin secretagogues aimed to enhance insulin release in patients with type 2 diabetes. GPR120 is the most enigmatic of the lipid responsive cell-surface receptors and its function remains to be established. It has been proposed to play a cytoprotective role in certain other cell types but it is unclear whether it fulfils a similar function in beta-cells.

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“…Free fatty acid receptors are expressed differentially, and they may play different functional roles. Immunoreactivity for GPR120 was found to be more abundant in the mouse large intestine, lung, and adipose tissues (26). High fat diet up-regulated GPR120 gene expression in skeletal muscles (27).…”

Section: Discussionmentioning

confidence: 99%