Ontology highlight
ABSTRACT:
SUBMITTER: La Rosa S
PROVIDER: S-EPMC4027250 | biostudies-literature | 2013 Oct
REPOSITORIES: biostudies-literature
La Rosa Salvatore S Benicchi Tiziana T Bettinetti Laura L Ceccarelli Ilaria I Diodato Enrica E Federico Cesare C Fiengo Pasquale P Franceschini Davide D Gokce Ozgun O Heitz Freddy F Lazzeroni Giulia G Luthi-Carter Ruth R Magnoni Letizia L Miragliotta Vincenzo V Scali Carla C Valacchi Michela M
ACS medicinal chemistry letters 20130808 10
Here, we describe the selection and optimization of a chemical series active in both a full-length and a fragment-based Huntington's disease (HD) assay. Twenty-four thousand small molecules were screened in a phenotypic HD assay, identifying a series of compounds bearing a 3-hydroxy-3-trifluoromethylpyrazole moiety as able to revert the toxicity induced by full-length mutant Htt by up to 50%. A chemical exploration around the series led to the identification of compound 4f, which demonstrated to ...[more]