The First-in-Class UBA1 Inhibitor, TAK-243, in Combination With Radiotherapy for YAP1 and BEND3 Biomarker-Defined Small Cell Lung Cancer

S Majeed, M Aparnathi, L Song,J Weiss, V Venkatasubramanian,K C J Nixon, R Barayan,V Philip,V Sugumar,S H Barghout,J D Pearson,R Bremner,A Schimmer, M Tsao,G Liu,B H Lok

INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS（2021）

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摘要

Our results demonstrated that inhibiting the UPS using a selective UBA1 inhibitor, TAK-243, is an effective anti-cancer strategy for SCLC. We determined a distinct transcriptomic-stratified (YAP1 and BEND3) population of SCLC that is sensitive to UBA1-inhibition therapy with TAK-243 as a single agent and a radiosensitizer.

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