Glycogen Synthase Kinase 3 (GSK 3) Targeted Therapy and Imaging
Glycogen synthase kinase 3 (GSK 3) is associated with various key biological processes, including glucose regulation, apoptosis, protein synthesis, cell signaling, cellular transport, gene transcription, proliferation, and intracellular communication. Accordingly, GSK 3 has been implicated in a wide variety of diseases and specifically targeted for both therapeutic and imaging applications by a large number of academic laboratories and pharmaceutical companies. Here, we review the structure, function, expression levels, and ligand binding properties of GSK 3 and its connection to various diseases. A selected list of highly potent GSK 3 inhibitors, with IC50 <20 nM for adenosine triphosphate (ATP) competitive inhibitors and IC50 <5 mM for non ATP competitive inhibitors, were analyzed for structure activity relationships. Furthermore, ubiquitous expression of GSK 3 and its possible impact on therapy and imaging are also highlighted. Finally, a rational perspective and possible route to selective and effective GSK 3 inhibitors is discussed.
Theranostics