Developing glycogen Synthase Kinase-3 Beta (GSK3b) Inhibitors for Psychiatric Disorder

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:shadow2100
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  The serine/threonine kinase glycogen synthase kinase-3 beta (GSK-3b) is a known master regulator for several cellular pathways that include insulin signaling and glycogen synthesis,neurotrophic factor signaling,Wnt signaling,neurotransmitter signaling and microtubule dynamics.This enzyme has been shown to have a critical role in neuronal functions and has been implicated in multiple neuronal disorders including Alzheimers disease and bipolar disorder.The majority of the existing chemical inhibitors compete for the ATP-binding site of GSK-3b and inhibit additional kinases,while the two known structural series ofATP-noncompetitive inhibitors have suboptimal pharmacological properties that limit their use.This presentation would offer a brief overview of GSk3b function in psychiatric disorders,its existing inhibitors,and would discuss the on-going efforts in developing HTS ready assays to potentially identify small molecules targeting the allosteric sites of GSK-3b.
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