2017
BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells
Sun B, Fiskus W, Qian Y, Rajapakshe K, Raina K, Coleman KG, Crew AP, Shen A, Saenz DT, Mill CP, Nowak AJ, Jain N, Zhang L, Wang M, Khoury JD, Coarfa C, Crews CM, Bhalla KN. BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells. Leukemia 2017, 32: 343-352. PMID: 28663582, DOI: 10.1038/leu.2017.207.Peer-Reviewed Original ResearchConceptsMantle cell lymphoma cellsMCL cellsCell lymphoma cellsARV-825ARV-771Lymphoma cellsGreater survival improvementSuperior preclinical activityCDK4/6 inhibitor palbociclibNuclear factor-κB (NF-κB) target genesExtraterminal protein inhibitorSurvival improvementInhibitor palbociclibPreclinical activityCDKN1A/p21Inhibitor treatmentSuperior pharmacological propertiesVivo growthCyclin D1Pharmacological propertiesProtein expressionMore apoptosisVivo evaluationIncomplete inhibitionC-Myc
2008
Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer
Rodriguez-Gonzalez A, Cyrus K, Salcius M, Kim K, Crews CM, Deshaies RJ, Sakamoto KM. Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer. Oncogene 2008, 27: 7201-7211. PMID: 18794799, PMCID: PMC5573236, DOI: 10.1038/onc.2008.320.Peer-Reviewed Original ResearchMeSH KeywordsAntineoplastic AgentsBlotting, WesternBreast NeoplasmsCell CycleCell Line, TumorCell ProliferationDihydrotestosteroneDrug Delivery SystemsEstradiolEstrogen Receptor alphaFemaleFlow CytometryHumansHypoxia-Inducible Factor 1, alpha SubunitMaleNeoplasms, Hormone-DependentProstatic NeoplasmsProteasome Endopeptidase ComplexReceptors, AndrogenReceptors, SteroidRecombinant Fusion ProteinsUbiquitinationConceptsBreast cancer cellsProstate cancer cellsCancer cellsAndrogen-dependent prostate cancer cellsHormone-dependent cell linesEstrogen-independent breast cancer cellsEstrogen-dependent breast cancer cellsHormone receptorsHormone-dependent breastG1 arrestDegradation of ERαSteroid hormone receptorsERα expressionProgesterone receptorAndrogen receptorProstate cancerEstrogen receptorCyclin D1Retinoblastoma phosphorylationReceptorsCell linesERαBreastProliferationProteasome-dependent manner