Insights to the emerging potential of glucokinase activators as antidiabetic agent.

The glucokinase enzyme (belongs to the hexokinase family) is present in liver cells and β-cells of the pancreas. Glucokinase acts as a catalyst in the conversion of glucose-6-phosphate from glucose which is rate-limiting step in glucose metabolism. Glucokinase becomes malfunctional or remains inactivated in diabetes. Glucokinase activators are compounds that bind at the allosteric site of the glucokinase enzyme and activate it. This article highlights the patent and recent research papers history with possible SAR from year 2014-2023. The data comprises the discussion of novel chemotypes (GKAs) that are being targeted for drug development and entered into clinical trials. GK activators have attracted massive interest since successful results have been reported from clinical trials data.