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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Chemistry, Pharmaceutical / methods*
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Combinatorial Chemistry Techniques
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Drug Design
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Drug Discovery
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Drug Evaluation, Preclinical
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Humans
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Huntingtin Protein
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Structure
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Nerve Tissue Proteins / antagonists & inhibitors*
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Nuclear Proteins / antagonists & inhibitors*
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Peptides / chemistry
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Quinazolines / chemistry*
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Structure-Activity Relationship
Substances
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HTT protein, human
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Huntingtin Protein
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Nerve Tissue Proteins
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Nuclear Proteins
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Peptides
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Quinazolines
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polyglutamine