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DYRK1A inhibition and cognitive rescue in a Down syndrome mouse model are induced by new fluoro-DANDY derivatives.

Abstract：

:Inhibition of DYRK1A kinase, produced by chromosome 21 and consequently overproduced in trisomy 21 subjects, has been suggested as a therapeutic approach to treating the cognitive deficiencies observed in Down syndrome (DS). We now report the synthesis and potent DYRK1A inhibitory activities of fluoro derivatives of 3,5-di(polyhydroxyaryl)-7-azaindoles (F-DANDYs). One of these compounds (3-(4-fluorophenyl)-5-(3,4-dihydroxyphenyl)-1H-pyrrolo[2,3-b]pyridine, 5a) was selected for in vivo studies of cognitive rescuing effects in a standard mouse model of DS (Ts65Dn line). Using the Morris water maze task, Ts65Dn mice treated i.p. with 20 mg/kg of 5a performed significantly better than Ts65Dn mice treated with placebo, confirming the promnesiant effect of 5a in the trisomic mice. Overall, these results demonstrate for the first time that selective and competitive inhibition of DYRK1A kinase by the F-DANDY derivative 5a may provide a viable treatment strategy for combating the memory and learning deficiencies encountered in DS.

journal_name

Sci Rep

journal_title

Scientific reports

authors

Neumann F,Gourdain S,Albac C,Dekker AD,Bui LC,Dairou J,Schmitz-Afonso I,Hue N,Rodrigues-Lima F,Delabar JM,Potier MC,Le Caër JP,Touboul D,Delatour B,Cariou K,Dodd RH

doi

10.1038/s41598-018-20984-z

subject

Has Abstract

pub_date

2018-02-12 00:00:00

pages

2859

issue

1

issn

2045-2322

pii

10.1038/s41598-018-20984-z

journal_volume

8

pub_type

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