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• W2499620239 abstract "DYRK1A is important in neuronal development and function, and its excessive activity is considered a significant pathogenic factor in Down syndrome and Alzheimer's disease. Thus, inhibition of DYRK1A has been suggested to be a new strategy to modify the disease. Very few compounds, however, have been reported to act as inhibitors, and their potential clinical uses require further evaluation. Here, we newly identify CX-4945, the safety of which has been already proven in the clinical setting, as a potent inhibitor of DYRK1A that acts in an ATP-competitive manner. The inhibitory potency of CX-4945 on DYRK1A (IC50=6.8 nM) in vitro was higher than those of harmine, INDY, and proINDY, which are the well-known potent inhibitors of DYRK1A. CX-4945 effectively reverses the aberrant phosphorylation of Tau, amyloid precursor protein (APP), and presenilin 1 (PS1) in mammalian cells. To our surprise, feeding with CX-4945 significantly restored the neurological and phenotypic defects induced by the overexpression of minibrain, an ortholog of human DYRK1A, in the Drosophila model. Moreover, oral administration of CX-4945 acutely suppressed Tau hyperphosphorylation in the hippocampus of DYRK1A-overexpressing mice. Our research results demonstrate that CX-4945 is a potent DYRK1A inhibitor, and also suggest its therapeutic potential for DYRK1A-associated diseases." @default.
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• W2499620239 date "2016-01-01" @default.
• W2499620239 modified "2023-10-17" @default.
• W2499620239 title "A chemical with proven clinical safety restores Down syndrome-related phenotypes via DYRK1A inhibition" @default.
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• W2499620239 doi "https://doi.org/10.1242/dmm.025668" @default.
• W2499620239 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5007978" @default.
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