A First-in-Class TWIST1 Inhibitor with Activity in Oncogene-Driven Lung Cancer
Yochum Z, Cades J, Mazzacurati L, Neumann N, Khetarpal S, Chatterjee S, Wang H, Attar M, Huang E, Chatley S, Nugent K, Somasundaram A, Engh J, Ewald A, Cho Y, Rudin C, Tran P, Burns T. A First-in-Class TWIST1 Inhibitor with Activity in Oncogene-Driven Lung Cancer. Molecular Cancer Research 2017, 15: 1764-1776. PMID: 28851812, PMCID: PMC5712248, DOI: 10.1158/1541-7786.mcr-17-0298.Peer-Reviewed Original ResearchConceptsOncogene-driven NSCLCTwist1 functionPatient-derived xenograft mouse modelsMarked anti-tumor activityEpithelial-mesenchymal transition transcription factorsNon-small cell lung cancer tumorigenesisSolid tumor malignanciesSingle-cell disseminationLung cancer tumorigenesisNovel therapeutic strategiesXenograft mouse modelCell lung cancer tumorigenesisEffects of harmineAnti-tumor activityConnectivity mapping analysisE2A proteinsNSCLC cellsNSCLC tumorigenesisMutant NSCLCAnalogs/derivativesMouse modelTherapeutic strategiesHarmine treatmentDimer partnerTherapeutic targetHigh expression of orphan nuclear receptor NR4A1 in a subset of ovarian tumors with worse outcome
Delgado E, Boisen M, Laskey R, Chen R, Song C, Sallit J, Yochum Z, Andersen C, Sikora M, Wagner J, Safe S, Elishaev E, Lee A, Edwards R, Haluska P, Tseng G, Schurdak M, Oesterreich S. High expression of orphan nuclear receptor NR4A1 in a subset of ovarian tumors with worse outcome. Gynecologic Oncology 2016, 141: 348-356. PMID: 26946093, PMCID: PMC5154956, DOI: 10.1016/j.ygyno.2016.02.030.Peer-Reviewed Original ResearchConceptsHigh-grade serous ovarian cancerWorse progression-free survivalProgression-free survivalOvarian cancer cell linesCancer cell linesFree survivalNuclear receptorsOvarian cancerOvarian cancer tissue samplesCell linesGrade serous ovarian cancerExpression of NR4A1Ovarian cancer pathogenesisStage of diseaseTCGA dataNormal ovarian tissuesSerous ovarian cancerCancer tissue samplesNormal ovarian samplesRelevant nuclear receptorsHGSOC cell linesCritical nuclear receptorOverexpression of NR4A1Orphan nuclear receptor NR4A1Ovarian tumors