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Scholar Results 1 - 10 of about 17 citing Tan: Selective small-molecule agonists of G protein–coupled receptor 40 promote glucose-depende.... (0.10 sec) 

The fatty acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat …


M Kebede, T Alquier, MG Latour, M Semache, C … - Diabetes, 2008 - Am Diabetes Assoc
OBJECTIVE—The G-protein–coupled receptor GPR40 is expressed in pancreatic β-cells and
is activated by long-chain fatty acids. Gene deletion studies have shown that GPR40
mediates, at least in part, fatty acid–amplification of glucose-induced insulin secretion ...
Cited by 13 - Related articles - All 4 versions

Lack of FFAR1/GPR40 Does Not Protect Mice From High-Fat Diet–Induced …


H Lan, LM Hoos, L Liu, G Tetzloff, W Hu, SJ … - Diabetes, 2008 - Am Diabetes Assoc
OBJECTIVE—FFAR1/GPR40 is a G-protein–coupled receptor expressed predominantly in pancreatic
islets mediating free fatty acid–induced insulin secretion. However, the physiological role of FFAR1
remains controversial. It was previously reported that FFAR1 knockout (Ffar1 −/− ) mice ...
Cited by 9 - Related articles - All 5 versions

International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1,-2, and- …

- pubget.com [PDF] 
LA Stoddart, NJ Smith, G Milligan - Pharmacological reviews, 2008 - ASPET
Identification of G protein-coupled receptors that are activated by free fatty acids has led to considerable
interest in their pharmacology and function because of the wide range of normal physiology and
disease states in which fatty acids have been implicated. Free fatty acid receptor (FFA) 1 ...
Cited by 9 - Related articles - All 5 versions

Glucolipotoxicity of the pancreatic beta cell


V Poitout, J Amyot, M Semache, B Zarrouki, D … - BBA-Molecular and Cell …, 2009 - Elsevier
The concept of glucolipotoxicity refers to the combined, deleterious effects of elevated
glucose, and fatty acid levels on pancreatic beta-cell function and survival. Significant progress
has been made in recent years towards a better understanding of the cellular and ...
Cited by 9 - Related articles - BL Direct - All 4 versions

Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate …


CS Sum, IG Tikhonova, S Costanzi, MC … - Journal of Biological …, 2009 - ASBMB
Activation of a number of class AG protein-coupled receptors (GPCRs) is thought to involve two
molecular switches, a rotamer toggle switch within the transmembrane domain and an ionic lock
at the cytoplasmic surface of the receptor; however, the mechanism by which agonist ...
Cited by 5 - Related articles - All 3 versions

The long-chain fatty acid receptor, GPR40, and glucolipotoxicity: investigations …


R Brownlie, R Mayers, J Pierce, A Marley, … - Biochemical Society …, 2008 - biochemsoctrans.org
GPR40 (G-protein-coupled receptor 40) has been shown to be a physiologically relevant receptor
for long-chain fatty acids. It is a family A G-protein-coupled receptor highly expressed in the
β-cell where it increases insulin secretion by signalling via G q and phospholipase C. ...
Cited by 5 - Related articles - Cached - All 4 versions

Conserved polar residues in transmembrane domains V, VI, and VII of free fatty …

- jbc.org
LA Stoddart, NJ Smith, L Jenkins, AJ Brown, G … - Journal of Biological …, 2008 - ASBMB
FFA2 and FFA3 are closely related G protein-coupled receptors that bind and respond to short
chain fatty acids. (FFA2 and FFA3 are the provisional International Union of Pharmacology designations
for the receptors previously called GPR43 and GPR41, respectively.) Sequence ...
Cited by 4 - Related articles - All 3 versions

Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 …


G Milligan, LA Stoddart, NJ Smith - British Journal of …, 2009 - interscience.wiley.com
The free fatty acid receptors FFA2 and FFA3 are recently de-orphanized G protein-coupled receptors
that share a group of short-chain free fatty acids as endogenous ligands. The expression of FFA2
and FFA3 by immune cells, in parts of the gastro-intestinal tract and by white adipocytes ...
Cited by 1 - Related articles - All 4 versions

Molecular Pharmacology of Promiscuous Seven Transmembrane Receptors …

- pbrc.edu [PDF] 
P Wellendorph, LD Johansen, H Brauner-Osborne - Molecular Pharmacology, 2009 - ASPET
A number of highly promiscuous seven transmembrane (7TM) receptors have been cloned and
characterized within the last few years. It is noteworthy that many of these receptors are activated
broadly by amino acids, proteolytic degradation products, carbohydrates, or free fatty ...
Cited by 1 - Related articles - All 5 versions

The action and mode of binding of thiazolidinedione ligands at free fatty acid …


NJ Smith, LA Stoddart, NM Devine, L Jenkins, G … - Journal of Biological …, 2009 - ASBMB
The endogenous ligands for free fatty acid receptor 1 (FFA1) are medium and longer chain free
fatty acids. However, a range of selective, small molecule ligands have recently been developed
as tool compounds to explore the therapeutic potential of this receptor, whereas clinically ...
Cited by 1 - Related articles - All 4 versions


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