Article
Kinome Reprogramming Is a Targetable Vulnerability in ESR1 Fusion-Driven Breast Cancer.
Cancer research - 2 Oct 2023
Gou Xuxu, Kim Beom-Jun, Anurag Meenakshi, Lei Jonathan T, Young Meggie N, Holt Matthew V, Fandino Diana, Vollert Craig T, Singh Purba, Alzubi Mohammad A, Malovannaya Anna, Dobrolecki Lacey E, Lewis Michael T, Li Shunqiang, Foulds Charles E, Ellis Matthew J
Abstract excerpt
Transcriptionally active ESR1 fusions (ESR1-TAF) are a potent cause of breast cancer endocrine therapy (ET) resistance. ESR1-TAFs are not directly druggable because the C-terminal estrogen/anti-estrogen-binding domain is replaced with translocated in-frame partner gene sequences that confer constitutive transactivation. To discover alternative treatments, a mass spectrometry (MS)-based kinase inhibitor pulldown...
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