Activator or inhibitor? GSK-3 as a new drug target

Fumi Takahashi

Research output: Contribution to journalComment/debate

112 Citations (Scopus)

Abstract

Glycogen synthase kinase-3 (GSK-3) is a cytoplasmic serine/threonine protein kinase that phosphorylates and inhibits glycogen synthase, thereby inhibiting glycogen synthesis from glucose. However, this serine/threonine kinase is now known to regulate numerous cellular processes through a number of signaling pathways important for cell proliferation, stem cell renewal, apoptosis and development. Because of these diverse roles, malfunction of this kinase is also known to be involved in the pathogenesis of human diseases, such as nervous system disorders, diabetes, bone formation, inflammation, cancer and heart failure. Therefore, GSK-3 is recognized as an attractive target for the development of new drugs. The present review summarizes the roles of GSK-3 in the insulin, Wnt/bcatenin and hedgehog signaling pathways including the regulation of their activities. The roles of GSK-3 in the development of human diseases within the context of its participation in various signaling pathways are also summarized. Finally, the possibility of new drug development targeting this kinase is discussed with recent information about inhibitors and activators of GSK-3.

Original languageEnglish
Pages (from-to)191-199
Number of pages9
JournalBiochemical Pharmacology
Volume86
Issue number2
DOIs
Publication statusPublished - Jan 1 2013

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Glycogen Synthase Kinase 3
Pharmaceutical Preparations
Protein-Serine-Threonine Kinases
Phosphotransferases
Osteitis
Glycogen Synthase
Cell proliferation
Neurology
Human Development
Drug Delivery Systems
Medical problems
Nervous System Diseases
Stem cells
Glycogen
Osteogenesis
Bone
Heart Failure
Cell Proliferation
Insulin
Apoptosis

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Pharmacology

Cite this

Activator or inhibitor? GSK-3 as a new drug target. / Takahashi, Fumi.

In: Biochemical Pharmacology, Vol. 86, No. 2, 01.01.2013, p. 191-199.

Research output: Contribution to journalComment/debate

Takahashi, Fumi. / Activator or inhibitor? GSK-3 as a new drug target. In: Biochemical Pharmacology. 2013 ; Vol. 86, No. 2. pp. 191-199.
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