title: Potent inhibitors of Huntingtin protein aggregation in a cell-based assay.
abstract: A quinazoline that decreases polyglutamine aggregate burden in a cell-based assay was identified from a high-throughput screen of a chemical-compound library, provided by the NIH Molecular Libraries Small Molecule Repository (MLSMR). A structure and activity study yielded leads with submicromolar potency.
authors.affiliation: Division of Experimental Therapeutics, Department of Medicine, Columbia University, 630 West 168th Street, New York, NY 10032, USA.
authors.forename: Alison
authors.initials: A
authors.lastname: Rinderspacher
authors.forename: Maria Laura
authors.initials: ML
authors.lastname: Cremona
authors.forename: Yidong
authors.initials: Y
authors.lastname: Liu
authors.forename: Shi-Xian
authors.initials: SX
authors.lastname: Deng
authors.forename: Yuli
authors.initials: Y
authors.lastname: Xie
authors.forename: Gangli
authors.initials: G
authors.lastname: Gong
authors.forename: Nathalie
authors.initials: N
authors.lastname: Aulner
authors.forename: Udo
authors.initials: U
authors.lastname: Többen
authors.forename: Katherine
authors.initials: K
authors.lastname: Myers
authors.forename: Caty
authors.initials: C
authors.lastname: Chung
authors.forename: Monique
authors.initials: M
authors.lastname: Andersen
authors.forename: Dusica
authors.initials: D
authors.lastname: Vidović
authors.forename: Stephan
authors.initials: S
authors.lastname: Schürer
authors.forename: Lars
authors.initials: L
authors.lastname: Brandén
authors.forename: Ai
authors.initials: A
authors.lastname: Yamamoto
authors.forename: Donald W
authors.initials: DW
authors.lastname: Landry
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D006801:Humans; D000071058:Huntingtin Protein; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors*; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors*; D010455:Peptides / Q000737:chemistry; D011799:Quinazolines / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: C086055:HTT protein, human; D000071058:Huntingtin Protein; D009419:Nerve Tissue Proteins; D009687:Nuclear Proteins; D010455:Peptides; D011799:Quinazolines; C097188:polyglutamine