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ETS transcription factors as emerging drug targets in cancer.
Medicinal Research Reviews ( IF 13.3 ) Pub Date : 2019-03-29 , DOI: 10.1002/med.21575
Michael Hsing 1 , Yuzhuo Wang 1 , Paul S Rennie 1 , Michael E Cox 1 , Artem Cherkasov 1
Affiliation  

The ETS family of proteins consists of 28 transcription factors, many of which have been implicated in development and progression of a variety of cancers. While one family member, ERG, has been rigorously studied in the context of prostate cancer where it plays a critical role, other ETS factors keep emerging as potential hallmark oncodrivers. In recent years, numerous studies have reported initial discoveries of small molecule inhibitors of ETS proteins and opened novel avenues for ETS‐directed cancer therapies. This review summarizes the state of the art data on therapeutic targeting of ETS family members and highlights the corresponding drug discovery strategies.

中文翻译:

ETS转录因子是癌症中新兴的药物靶标。

ETS蛋白质家族由28个转录因子组成,其中许多因子与多种癌症的发生和发展有关。虽然在前列腺癌中起着至关重要作用的一位家庭成员ERG进行了严格的研究,但其他ETS因素仍在不断涌现,成为潜在的致癌因素。近年来,许多研究报告了ETS蛋白小分子抑制剂的初步发现,并为ETS导向的癌症治疗开辟了新途径。这篇综述总结了以ETS家族成员为治疗靶点的最新数据,并重点介绍了相应的药物发现策略。
更新日期:2019-03-29
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