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EGFR as therapeutic target to develop new generation tyrosine kinase inhibitors against breast cancer: A critical review
Results in Chemistry Pub Date : 2024-04-10 , DOI: 10.1016/j.rechem.2024.101490
Ruby Mariam Raju , Jeffin Joy A , Raghavendra Nulgumnalli Manjunathaiah , Antony Justin , B.R. Prashantha Kumar

Epidermal Growth Factor Receptor is a multifunctional receptor and is an important member of tyrosine kinase family. Investigation on mechanism of tumour progression and its suppression has identified prominent role of EGFR, which was the first identified amongst its family. EGFR has various cellular functions but aberration of the receptor results in tumour development. About half of the breast cancer cases overexpresses EGFR, making it as an appropriate target for discovery of molecular based targeted therapeutics i.e., EGFR inhibitors. This review focusses on the structural features, signaling pathways and role of EGFR in breast cancer. In addition to this, the recent developments of TKIs targeting EGFR are discussed along with the structural activity relationships. Also, the article highlights on the tyrosine kinase inhibitors that are under clinical study and patents.

中文翻译:

EGFR 作为开发新一代酪氨酸激酶抑制剂治疗乳腺癌的治疗靶点:一项严格审查

表皮生长因子受体是一种多功能受体,是酪氨酸激酶家族的重要成员。对肿瘤进展及其抑制机制的研究发现了EGFR的显着作用,这是其家族中首次发现的。 EGFR 具有多种细胞功能,但受体的异常会导致肿瘤的发生。大约一半的乳腺癌病例过度表达 EGFR,使其成为发现基于分子的靶向治疗(即 EGFR 抑制剂)的合适靶点。本综述重点关注 EGFR 在乳腺癌中的结构特征、信号通路和作用。除此之外,还讨论了针对 EGFR 的 TKI 的最新进展以及结构活性关系。此外,本文还重点介绍了正在进行临床研究和专利的酪氨酸激酶抑制剂。
更新日期:2024-04-10
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