Paola Conforti, Chiara Zuccato, Germano Gaudenzi, Alessandro Ieraci, Stefano Camnasio, Noel J. Buckley, Cesare Mutti, Franco Cotelli, Alessandro Contini and Elena Cattaneo Binding of the repressor complex REST-mSIN3b by small molecules restores neuronal gene transcription in Huntington's disease models Journal of Neurochemistry 127
Dysregulation of REST and its target genes have been implicated in Huntington's disease. We have coupled structured-based virtual screening approaches to biological assays and selected molecules that interfere with the repressor complex REST-mSIN3b. In particular, at the non-toxic dose, compound C91 is able to increase neuronal gene transcription and to reverse low Bdnf mRNA levels in HD models.
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