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Updated: Mar 28, 2026

Modeling an Enzyme Active Site using Molecular Visualization Freeware
Published on: December 25, 2021
Structure-Activity Relationship of Azaindole-Based Glucokinase Activators
Attila Paczal1, Balázs Bálint1, Csaba Wéber1
1Servier Research Institute of Medicinal Chemistry , Záhony u. 7., H-1031 Budapest, Hungary.
Abstract:
7-Azaindole has been identified as a novel bidentate anchor point for allosteric glucokinase activators. A systematic investigation around three principal parts of the new small molecule glucokinase activators led to a robust SAR in agreement with structural data that also helped to assess the conformational flexibility of the allosteric activation site. The increase in glucose uptake resulting from glucokinase activation in hepatocytes in vitro translated into the efficient lowering of glucose levels in vivo with the best compounds.
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