Recent Advances in Epidermal Growth Factor Receptor Inhibitors (EGFRIs) andtheir Role in the Treatment of Cancer: A Review

癌症研究 表皮生长因子受体 ERBB3型 受体酪氨酸激酶 酪氨酸激酶 生物 表皮生长因子受体抑制剂 癌症 表皮生长因子 埃罗替尼 生长因子受体 靶向治疗 血管生成 信号转导 ERBB4公司 血小板源性生长因子受体 医学 生长因子 受体 细胞生物学 内科学
作者
Aziz Unnisa,Ananda Kumar Chettupalli,Talib Hussain,Mohammad Amjad Kamal
出处
期刊:Anti-cancer Agents in Medicinal Chemistry [Bentham Science Publishers]
卷期号:22 (20): 3370-3381 被引量:30
标识
DOI:10.2174/1871520622666220408090541
摘要

Tyrosine kinases are known to play a role in tumour growth and proliferation, and they have become common drug targets. Tyrosine kinase inhibitors (TKIs) prohibit associated kinases from phosphorylating tyrosine residues in their substrates, preventing downstream signaling pathways from being activated. Multiple robust and well-tolerated TKIs targeting single or multiple targets, including EGFR, ALK, ROS1, HER2, NTRK, VEGFR, RET, MET, MEK, FGFR, PDGFR, and KIT, have been developed over the last two decades, contributing to our understanding of precision cancer medicine based on a patient's genetic alteration profile. The epidermal growth factor receptor (EGFR) family consists of four transmembrane tyrosine kinases (EGFR1/ErbB1, Her2/ErbB2, Her3/ErbB3, and Her4/ErbB4) and thirteen polypeptide ligands produced by them. Multiple solid tumours, including breast, pancreatic, head and neck, kidney, vaginal, renal, colon, and non-small cell lung cancer, overexpress EGFRs. Overexpression of these genes stimulates downstream signaling channels, causing cell proliferation, differentiation, cell cycle progression, angiogenesis, cell motility, and apoptosis inhibition. EGFRs' high expression and/or adaptive activation coincide with the pathogenesis and development of many tumours, making them appealing candidates for both diagnosis and therapy. Several strategies for targeting these receptors and/or the EGFR-mediated effects in cancer cells have been established. The majority of methods include the development of anti-EGFR antibodies and/or small-molecule EGFR inhibitors. This review presents the recent advances in EGFR TKIs and their role in the treatment of cancer.
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