Benzothiophenone Derivatives Targeting Mutant Forms of Estrogen Receptor-α in Hormone-Resistant Breast Cancers

Benzothiophenone Derivatives Targeting Mutant Forms of Estrogen Receptor-α in Hormone-Resistant Breast Cancers

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, whi...

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Bibliographic Details
Main Authors: Kriti Singh, Ravi S. N. Munuganti, Nada Lallous, Kush Dalal, Ji Soo Yoon, Aishwariya Sharma, Takeshi Yamazaki, Artem Cherkasov, Paul S. Rennie
Format: Article
Language:English
Published: MDPI AG 2018-02-01
Series:International Journal of Molecular Sciences
Subjects:
breast cancer
estrogen receptor
hormone resistance
small molecule inhibitors
mutations
in silico modelling
activation function-2 (AF2) site
Online Access:http://www.mdpi.com/1422-0067/19/2/579

Internet

http://www.mdpi.com/1422-0067/19/2/579

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