Literature summary for 2.7.11.31 extracted from

Zhang, F.; Dey, D.; Braenstroem, R.; Forsberg, L.; Lu, M.; Zhang, Q.; Sjoeholm, A.
BLX-1002, a novel thiazolidinedione with no PPAR affinity, stimulates AMP-activated protein kinase activity, raises cytosolic Ca2+, and enhances glucose-stimulated insulin secretion in a PI3K-dependent manner (2009), Am. J. Physiol. Cell Physiol., 296, C346-C354.

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Activating Compound

Activating Compound	Comment	Organism	Structure
BLX-1002	has no affinity to peroxisome proliferator-activated receptors (PPAR), stimulation of beta-cells with BLX-1002 induces activation of AMPK at high glucose. BLX-1002 selectively potentiates insulin secretion induced by high glucose in normal and diabetic islets in a PI3K-dependent manner. This effect is associated with an increased cytoplasmic free Ca2+ concentration mediated through Ca2+ mobilization, and an enhanced activation of AMPK	Mus musculus
BLX-1015	0.01 mM significantly enhances AMPK phosphorylation, to an extent similar to that of BLX-1002. Potentiates pioglitazone-, but not fenofibrate-induced insulin secretion	Mus musculus
metformin	stimulates AMPK, does not induce any significant change in glucose-stimulated insulin secretion	Mus musculus

Application

Application	Comment	Organism
drug development	the glucose-sensitive stimulatory impact of BLX-1002 on beta-cell function associated with AMPK activation may translate into substantial clinical benefits of the drug in the management of type 2 diabetes, by avoidance of hypoglycemia	Mus musculus

Inhibitors

Inhibitors	Comment	Organism	Structure
6-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-3-pyridin-4-yl-pyrrazolo[1,5-a]-pyrimidine	compound C, at a concentration of 0.02 mM, suppresses the glucose-stimulated rise in cytoplasmic free Ca2+ concentration by 75%, and the cytoplasmic free Ca2+ concentration response to BLX-1002 is also significantly suppressed	Mus musculus
glucose	AMPK activity is inhibited by high glucose	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Mus musculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
pancreatic beta cell	-	Mus musculus	-
pancreatic islet	-	Mus musculus	-

Synonyms

Synonyms	Comment	Organism
AMP-activated protein kinase	-	Mus musculus
AMPK	-	Mus musculus

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Release 2023.1 (January 2023)