2016
ARV-330: Androgen receptor PROTAC degrader for prostate cancer.
Neklesa T, Jin M, Crew A, Rossi A, Willard R, Dong H, Siu K, Wang J, Gordon D, Chen X, Ferraro C, Crews C, Coleman K, Winkler J. ARV-330: Androgen receptor PROTAC degrader for prostate cancer. Journal Of Clinical Oncology 2016, 34: 267-267. DOI: 10.1200/jco.2016.34.2_suppl.267.Peer-Reviewed Original ResearchAndrogen receptorAR mutationsProstate cancerTotal androgen receptorTreatment of miceAR protein levelsProstate cancer cellsGood pharmacokinetic propertiesPlasma PSAMetastatic diseaseNM R1881SC injectionAndrogen productionDisease progressionPSA expressionIntact miceTherapeutic effectCastrated miceVCaP cellsAnimal modelsProstate involutionTumor growthVivo efficacyPreclinical developmentPharmacokinetic properties
2015
Small‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging
Gustafson JL, Neklesa TK, Cox CS, Roth AG, Buckley DL, Tae HS, Sundberg TB, Stagg DB, Hines J, McDonnell DP, Norris JD, Crews CM. Small‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging. Angewandte Chemie International Edition 2015, 54: 9659-9662. PMID: 26083457, PMCID: PMC4547777, DOI: 10.1002/anie.201503720.Peer-Reviewed Original ResearchMeSH KeywordsAndrogen Receptor AntagonistsAntineoplastic AgentsBenzamidesCell Line, TumorCell ProliferationDrug Resistance, NeoplasmHumansHydrophobic and Hydrophilic InteractionsMaleNitrilesPhenylthiohydantoinPoint MutationProstateProstatic NeoplasmsProteolysisReceptors, AndrogenSmall Molecule LibrariesConceptsSelective androgen receptor degradersAndrogen receptorAR mutationsAndrogen-dependent prostate cancer cell lineSecond-generation AR antagonistsAR degradationProstate tumor cell proliferationProstate cancer cell linesAR target genesTumor cell proliferationAntitumor chemotherapeutic agentsCancer cell linesAR antagonistsChemotherapeutic agentsCell proliferationAR ligandsCell linesAntagonistTumor strategyResistance mechanismsReceptorsRecent studiesProliferationTarget genesDependent transcriptionSmall‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging
Gustafson J, Neklesa T, Cox C, Roth A, Buckley D, Tae H, Sundberg T, Stagg D, Hines J, McDonnell D, Norris J, Crews C. Small‐Molecule‐Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging. Angewandte Chemie 2015, 127: 9795-9798. DOI: 10.1002/ange.201503720.Peer-Reviewed Original ResearchSelective androgen receptor degradersAndrogen receptorAR mutationsAndrogen-dependent prostate cancer cell lineSecond-generation AR antagonistsAR degradationProstate tumor cell proliferationProstate cancer cell linesAR target genesTumor cell proliferationAntitumor chemotherapeutic agentsCancer cell linesAR antagonistsChemotherapeutic agentsCell proliferationAR ligandsCell linesAntagonistTumor strategyResistance mechanismsReceptorsRecent studiesProliferationTarget genesDependent transcription