Glycogen synthase kinase 3 beta (GSK-3β) is an attractive target for the treatment of psychiatric disorders and neurodegenerative diseases. Many GSK-3β inhibitors have been developed for the treatment of different central nervous system disorders. But, for an effective therapy, high IC50 values should be avoided and ATP-competition should be reduced during enzyme-compound binding. Studies suggested that ATP non-competitive GSK-3 inhibitors such covalent inhibitors and allosteric modulators are emerging as a promising approach with better efficacy and safety.
Despite of many GSK-3β inhibitors in clinical studies, many
challenges still remains. In a clinical study, certain adverse events caused by
off-target activity of GSK-3β inhibitors were determined after the screening of
compounds that bind to the ATP-competitive binding site conserved across a
broad range of kinases. Thus, there is an urgent need of development of GSK-3β
inhibitors that can selectively target individual pathways and differentiate
between the non-phosphorylated and phosphorylated GSK-3β.
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The report provides a comprehensive understanding of the
pipeline activities covering all drug candidates under various stages of
development, with detailed analysis of pipeline and clinical trials. Pipeline
analysis of drugs by phases includes product description and development
activities including information about clinical results, designations,
collaborations, licencing, grants, technology and others.
