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Eur J Med Chem. 2017 Jan 5;125:464-477. doi: 10.1016/j.ejmech.2016.09.058. Epub 2016 Sep 20.

Natural and synthetic bioactive inhibitors of glycogen synthase kinase.

Author information

1
Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India.
2
Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India. Electronic address: hhamid@jamiahamdard.ac.in.

Abstract

Glycogen synthase kinase-3 is a multi-functional serine-threonine kinase and is involved in diverse physiological processes, including metabolism, cell cycle, and gene expression by regulating a wide variety of known substrates like glycogen synthase, tau-protein and β-catenin. Aberrant GSK-3 has been involved in diabetes, inflammation, cancer, Alzheimer's and bipolar disorder. In this review, we present an overview of the involvement of GSK-3 in various signalling pathways, resulting in a number of adverse pathologies due to its dysregulation. In addition, a detailed description of the small molecule inhibitors of GSK-3 with different mode of action discovered or specifically developed for GSK-3 has been presented. Furthermore, some clues for the future optimization of these promising molecules to develop specific drugs inhibiting GSK-3, for the treatment of associated disease conditions have also been discussed.

KEYWORDS:

ATP; Alzheimer's disease; Diabetes; Glycogen synthase kinase; Kinases; Phosphorylation

PMID:
27689729
DOI:
10.1016/j.ejmech.2016.09.058
[Indexed for MEDLINE]

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