Article
Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition.
JCI insight - 8 Sept 2022
Udden Sm N, Wang Qian, Kumar Sunil, Malladi Venkat S, Wu Shwu-Yuan, Wei Shuguang, Posner Bruce A, Geboers Sophie, Williams Noelle S, Liu Yulun, Sharma Jayesh K, Mani Ram S, Malladi Srinivas, Parra Karla, Hofstad Mia, Raj Ganesh V, Larios Jose M, Jagsi Reshma, Wicha Max S, Park Ben Ho, Gupta Gaorav P, Chinnaiyan Arul M, Chiang Cheng-Ming, Alluri Prasanna G
Abstract excerpt
Acquired mutations in the ligand-binding domain (LBD) of the gene encoding estrogen receptor α (ESR1) are common mechanisms of endocrine therapy resistance in patients with metastatic ER+ breast cancer. The ESR1 Y537S mutation, in particular, is associated with development of resistance to most endocrine therapies used to treat breast cancer. Employing a high-throughput screen of nearly 1,200 Federal Drug...
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