2009
An AlphaScreen™-Based High-Throughput Screen to Identify Inhibitors of Hsp90-Cochaperone Interaction
Yi F, Zhu P, Southall N, Inglese J, Austin CP, Zheng W, Regan L. An AlphaScreen™-Based High-Throughput Screen to Identify Inhibitors of Hsp90-Cochaperone Interaction. SLAS DISCOVERY 2009, 14: 273-281. PMID: 19211782, PMCID: PMC3066041, DOI: 10.1177/1087057108330114.Peer-Reviewed Original ResearchConceptsImportant anticancer drug targetFirst high-throughput screenHigh-throughput screenChemical probesNovel anticancer drugsAnticancer drug targetSuch moleculesAnticancer drugsTPR2A domainDifferent interactionsCompoundsSmall molecule Hsp90 inhibitorsNovel typeSynthetic peptidesFurther optimizationDrug targetsC-terminal peptideAlphaScreen technologyPeptidesDMSOReported valuesMoleculesInteractionHsp90 inhibitorsBackground ratio
2008
A Novel Class of Small Molecule Inhibitors of Hsp90
Yi F, Regan L. A Novel Class of Small Molecule Inhibitors of Hsp90. ACS Chemical Biology 2008, 3: 645-654. PMID: 18785742, PMCID: PMC3282108, DOI: 10.1021/cb800162x.Peer-Reviewed Original ResearchMeSH KeywordsAnticarcinogenic AgentsBenzoquinonesCell Line, TumorCell ProliferationDrug Screening Assays, AntitumorHSP90 Heat-Shock ProteinsHumansLactams, MacrocyclicReceptor, ErbB-2ConceptsGrowth-promoting proteinsChaperone heat shock protein 90Unregulated cellular proliferationHeat shock protein 90Inhibition of Hsp90Hydrolysis of ATPHuman breast cancer cell lines BT474Small molecule inhibitorsBreast cancer cell line BT474Hsp90 functionMultichaperone complexCorrect foldingAlphaScreen technologyProtein 90Hsp90Cell deathMolecule inhibitorsCell line BT474ATP analogCellular proliferationProteinNovel classCochaperonesApplicable strategyAnticancer agents