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A slipped-CAG DNA-binding small molecule induces trinucleotide-repeat contractions in vivo
Journal article   Peer reviewed

A slipped-CAG DNA-binding small molecule induces trinucleotide-repeat contractions in vivo

Masayuki Nakamori, Gagan B Panigrahi, Stella Lanni, Terence Gall-Duncan, Hideki Hayakawa, Hana Tanaka, Jennifer Luo, Takahiro Otabe, Jinxing Li, Akihiro Sakata, …
Nature genetics, Vol.52(2), pp.146-159
02/2020
DOI: 10.1038/s41588-019-0575-8
PMCID: PMC7043212
PMID: 32060489

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Abstract

In many repeat diseases, such as Huntington's disease (HD), ongoing repeat expansions in affected tissues contribute to disease onset, progression and severity. Inducing contractions of expanded repeats by exogenous agents is not yet possible. Traditional approaches would target proteins driving repeat mutations. Here we report a compound, naphthyridine-azaquinolone (NA), that specifically binds slipped-CAG DNA intermediates of expansion mutations, a previously unsuspected target. NA efficiently induces repeat contractions in HD patient cells as well as en masse contractions in medium spiny neurons of HD mouse striatum. Contractions are specific for the expanded allele, independently of DNA replication, require transcription across the coding CTG strand and arise by blocking repair of CAG slip-outs. NA-induced contractions depend on active expansions driven by MutSβ. NA injections in HD mouse striatum reduce mutant HTT protein aggregates, a biomarker of HD pathogenesis and severity. Repeat-structure-specific DNA ligands are a novel avenue to contract expanded repeats.
Mutation Animals Corpus Striatum - drug effects Disease Models, Animal DNA - metabolism DNA Mismatch Repair - drug effects DNA Replication - drug effects Humans Huntingtin Protein - genetics Huntingtin Protein - metabolism Huntington Disease - drug therapy Huntington Disease - genetics Huntington Disease - pathology Male Mice Mice, Transgenic Microsatellite Instability Naphthyridines - pharmacology Quinolones - pharmacology Ribonucleases - metabolism TATA-Box Binding Protein - genetics Transcription, Genetic Trinucleotide Repeat Expansion - drug effects

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