2014
TP53 mutation‐correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53‐mutated breast cancers
Győrffy B, Bottai G, Lehmann-Che J, Kéri G, Őrfi L, Iwamoto T, Desmedt C, Bianchini G, Turner NC, de Thè H, André F, Sotiriou C, Hortobagyi GN, Di Leo A, Pusztai L, Santarpia L. TP53 mutation‐correlated genes predict the risk of tumor relapse and identify MPS1 as a potential therapeutic kinase in TP53‐mutated breast cancers. Molecular Oncology 2014, 8: 508-519. PMID: 24462521, PMCID: PMC5528634, DOI: 10.1016/j.molonc.2013.12.018.Peer-Reviewed Original ResearchConceptsBreast cancerTP53 mutation statusPrognostic valueBC cellsMutation statusER-negative breast cancerDifferent BC cell linesFuture clinical trialsSignificant prognostic markerPotential therapeutic targetBC cell linesType of treatmentNeoadjuvant chemotherapyBC patientsClinical behaviorPrognostic markerClinical trialsConventional chemotherapyEstrogen receptorPotent small molecule inhibitorsTumor relapseSmall molecule inhibitorsTherapeutic targetClinical relevanceTP53 status
2011
Molecular Markers of Response to Treatment for Melanoma
Sznol M. Molecular Markers of Response to Treatment for Melanoma. The Cancer Journal 2011, 17: 127-133. PMID: 21427556, DOI: 10.1097/ppo.0b013e318212dd5a.Peer-Reviewed Original ResearchConceptsImmune therapyAnti-tumor immune responseInitial high response rateStandard of careFraction of patientsUseful predictive biomarkerHigh response rateMost patientsMetastatic melanomaPredictive biomarkersClinical activityImmune responseIndividual patientsPotent small molecule inhibitorsDurable benefitMultiple active agentsSmall molecule inhibitorsResponse ratePatientsMutant BRAFOverall populationTherapyMolecule inhibitorsMelanomaTumors
1998
General Solid-Phase Synthesis Approach To Prepare Mechanism-Based Aspartyl Protease Inhibitor Libraries. Identification of Potent Cathepsin D Inhibitors
Lee C, Kick E, Ellman J. General Solid-Phase Synthesis Approach To Prepare Mechanism-Based Aspartyl Protease Inhibitor Libraries. Identification of Potent Cathepsin D Inhibitors. Journal Of The American Chemical Society 1998, 120: 9735-9747. DOI: 10.1021/ja981812m.Peer-Reviewed Original ResearchSolid-phase synthesis approachSynthesis approachSolid-phase synthesisExpedient solid-phase synthesisProtease inhibitor libraryAvailable precursorsSynthesis sequenceSeparate compoundsStereoselective reductionPotent small molecule inhibitorsSmall molecule inhibitorsOverall yieldDiverse functionalitiesEnzyme classesProtease targetsMolecule inhibitorsGeneral design principlesAspartyl protease inhibitorsCathepsin D inhibitorInhibitor libraryPure inhibitorGeneral methodBondsAmino acidsCompounds
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