Putative therapeutic agents for the learning and memory deficits of people with Down syndrome

Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes significant learning and memory deficits in DS-model mice. Thus far, no mechanism-based drug has been developed to address this. After a combination of in silico and in vitro screenings, two DYRK1A inhibitors were isolated that are active in a cell-based assay. Further optimization could lead to a novel drug discovery that could address DS learning and memory deficits.

Graphical abstractA novel series of DYRK1A inhibitors were identified by combination of in silico screening, in vitro assay, and cell-based screenings.Figure optionsDownload full-size imageDownload as PowerPoint slide