Because glucokinase is a metabolic sensor involved in the regulated release of insulin, we have investigated the acute actions of novel glucokinase activator compound 50 (GKA50) on islet function. Insulin secretion was determined by enzyme-linked immunosorbent assay, and microfluorimetry with fura-2 was used to examine We show that GKA50 is a glucose-like activator of ␤-cell metabolism in rodent and human islets and a Ca 2؉ -dependent modulator of insulin secretion.

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