Article
Benzothiophenone Derivatives Targeting Mutant Forms of Estrogen Receptor-α in Hormone-Resistant Breast Cancers.
International journal of molecular sciences - 15 Feb 2018
Singh Kriti, Munuganti Ravi S N, Lallous Nada, Dalal Kush, Yoon Ji Soo, Sharma Aishwariya, Yamazaki Takeshi, Cherkasov Artem, Rennie Paul S
Abstract excerpt
Estrogen receptor-α positive (ERα⁺) breast cancers represent 75% of all invasive breast cancer cases, while de novo or acquired resistance to ER-directed therapy is also on the rise. Numerous factors contribute to this phenomenon including the recently-reported ESR1 gene mutations such as Y537S, which amplifies co-activator interactions with ERα and promotes constitutive activation of ERα function. Herein, we...
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