Enzalutamide: looking back at its preclinical discovery
Ha Y, Kim I. Enzalutamide: looking back at its preclinical discovery. Expert Opinion On Drug Discovery 2014, 9: 837-845. PMID: 24820058, DOI: 10.1517/17460441.2014.918947.Peer-Reviewed Original ResearchConceptsCastration-recurrent PCaFirst-line therapyProstate cancerClinical developmentCastration-recurrent prostate cancerStandard first-line therapyAndrogen-AR axisAR agonist activityMetastatic prostate cancerAR nuclear translocationSelective AR modulatorsFurther clinical studiesAndrogen receptor antagonistPre-clinical discoveryDrug clinical developmentSequential therapyOverall survivalTargeted agentsReceptor antagonistClinical studiesPreclinical discoveryNew agentsAR modulatorsAgonist activityFDA approvalProstate cancer bone metastases acquire resistance to androgen deprivation via WNT5A-mediated BMP-6 induction
Lee G, Kang D, Ha Y, Jung Y, Chung J, Min K, Kim T, Moon K, Chung J, Lee D, Kim W, Kim I. Prostate cancer bone metastases acquire resistance to androgen deprivation via WNT5A-mediated BMP-6 induction. British Journal Of Cancer 2014, 110: 1634-1644. PMID: 24518599, PMCID: PMC3960605, DOI: 10.1038/bjc.2014.23.Peer-Reviewed Original ResearchMeSH KeywordsAdultAndrogen AntagonistsAnilidesBone Morphogenetic Protein 6Bone NeoplasmsCell CommunicationCell Growth ProcessesCell Line, TumorHumansMaleMiddle AgedNeoplasm MetastasisNitrilesOrchiectomyProstatic Neoplasms, Castration-ResistantProto-Oncogene ProteinsReceptors, AndrogenRetrospective StudiesStromal CellsTosyl CompoundsWnt ProteinsWnt-5a ProteinConceptsCastration-resistant prostate cancerBone stromal cellsBone metastasesBone morphogenetic protein 6Castration resistanceCaP cell linesStromal cellsProstate cancerPrimary androgen deprivation therapyProstate-specific antigen progressionProstate cancer bone metastasisAndrogen-deprived mediumBone-tumor interactionAndrogen deprivation therapyFirst-line therapyCancer bone metastasisMetastatic prostate cancerAbsence of androgenAndrogen-depleted conditionsNF-κB pathwayCell linesPolymerase chain reaction arrayBMP-6 expressionAdvanced CaPDeprivation therapy