研究动态
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癌症靶向受体酪氨酸激酶的治疗进展。

Therapeutic advances of targeting receptor tyrosine kinases in cancer.

发表日期:2024 Aug 14
作者: Ciprian Tomuleasa, Adrian-Bogdan Tigu, Raluca Munteanu, Cristian-Silviu Moldovan, David Kegyes, Anca Onaciu, Diana Gulei, Gabriel Ghiaur, Hermann Einsele, Carlo M Croce
来源: Signal Transduction and Targeted Therapy

摘要:

受体酪氨酸激酶(RTK)是一类跨膜受体,由于其在癌症发病机制中的核心作用而在肿瘤学领域获得了显着的临床关注。基因改变,包括某些 RTK 的突变、扩增和过度表达,对于创造有利于肿瘤发展的环境至关重要。在他们的发现之后,广泛的研究揭示了 RTK 失调如何导致肿瘤发生,许多癌症亚型的增殖、存活和进展都依赖于异常的 RTK 信号传导。这些发现为旨在抑制癌症关键生物学途径的靶向治疗铺平了道路。因此,RTK 已成为抗癌治疗开发的主要靶点。在过去的二十年里,这导致了许多小分子酪氨酸激酶抑制剂 (TKI) 的合成和临床验证,这些抑制剂现已有效地用于治疗各种癌症类型。在这篇手稿中,我们的目标是提供对癌症背景下 RTK 的全面理解。我们探索了不同恶性肿瘤中特定受体的各种改变和过度表达,特别关注当前 RTK 抑制剂的检查,强调了它们作为潜在靶向治疗的作用。通过整合最新的研究结果和临床证据,我们试图阐明 RTK 在癌症生物学中的关键作用以及 RTK 抑制的治疗效果和有希望的治疗结果。© 2024。作者。
Receptor tyrosine kinases (RTKs), a category of transmembrane receptors, have gained significant clinical attention in oncology due to their central role in cancer pathogenesis. Genetic alterations, including mutations, amplifications, and overexpression of certain RTKs, are critical in creating environments conducive to tumor development. Following their discovery, extensive research has revealed how RTK dysregulation contributes to oncogenesis, with many cancer subtypes showing dependency on aberrant RTK signaling for their proliferation, survival and progression. These findings paved the way for targeted therapies that aim to inhibit crucial biological pathways in cancer. As a result, RTKs have emerged as primary targets in anticancer therapeutic development. Over the past two decades, this has led to the synthesis and clinical validation of numerous small molecule tyrosine kinase inhibitors (TKIs), now effectively utilized in treating various cancer types. In this manuscript we aim to provide a comprehensive understanding of the RTKs in the context of cancer. We explored the various alterations and overexpression of specific receptors across different malignancies, with special attention dedicated to the examination of current RTK inhibitors, highlighting their role as potential targeted therapies. By integrating the latest research findings and clinical evidence, we seek to elucidate the pivotal role of RTKs in cancer biology and the therapeutic efficacy of RTK inhibition with promising treatment outcomes.© 2024. The Author(s).