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JOURNAL OF MOLECULAR GRAPHICS & MODELLING (2010)
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JOURNAL OF ORGANIC CHEMISTRY (2010)
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
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DIABETES (2009)
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DIABETOLOGIA (2009)
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JOURNAL OF BIOLOGICAL CHEMISTRY (2009)
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DIABETES (2008)
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BRITISH JOURNAL OF PHARMACOLOGY (2006)
Synthesis and activity of small molecule GPR40 agonists
DM Garrido et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Reduction in voltage-gated K+ currents in primary cultured rat pancreatic β-cells by linoleic acids
DD Feng et al.
ENDOCRINOLOGY (2006)
Glucose-sensing mechanisms in pancreatic β-cells
PE MacDonald et al.
PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES (2005)
Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet β-cells:: mediation by PLC and L-type Ca2+ channel and link to insulin release
K Fujiwara et al.
AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM (2005)
Role of GPR40 in fatty acid action on the β cell line INS-1E
H Shapiro et al.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2005)
Interplay of Ca2+ and cAMP signaling in the insulin-secreting MIN6 β-cell line
LR Landa et al.
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The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse
R Steneberg et al.
CELL METABOLISM (2005)
Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
A Hirasawa et al.
NATURE MEDICINE (2005)
A highly Ca2+-sensitive pool of granules is regulated by glucose and protein kinases in insulin-secreting INS-1 cells
Y Yang et al.
JOURNAL OF GENERAL PHYSIOLOGY (2004)
Protein kinase activation increases insulin secretion by sensitizing the secretory machinery to Ca2+
QF Wan et al.
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The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
CP Briscoe et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2003)
Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40
Y Itoh et al.
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A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs
K Kotarsky et al.
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Pleiotropic effects of fatty acids on pancreatic beta-cells
EP Haber et al.
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Lipotoxicity in human pancreatic islets and the protective effect of metformin
R Lupi et al.
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Interactions between insulin resistance and insulin secretion in the development of glucose intolerance
MK Cavaghan et al.
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Roles of PPARs in health and disease
S Kersten et al.
NATURE (2000)
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