针对癌症受体酪氨酸激酶的治疗进展。

IF 40.8 1区 医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY Signal Transduction and Targeted Therapy Pub Date : 2024-08-14 DOI:10.1038/s41392-024-01899-w
Ciprian Tomuleasa, Adrian-Bogdan Tigu, Raluca Munteanu, Cristian-Silviu Moldovan, David Kegyes, Anca Onaciu, Diana Gulei, Gabriel Ghiaur, Hermann Einsele, Carlo M Croce
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引用次数: 0

摘要

受体酪氨酸激酶(RTKs)是一类跨膜受体,由于其在癌症发病机制中的核心作用,已在肿瘤学临床上获得了极大的关注。基因改变,包括某些 RTKs 的突变、扩增和过表达,对创造有利于肿瘤发展的环境至关重要。发现 RTK 后,大量研究揭示了 RTK 失调是如何导致肿瘤发生的,许多癌症亚型的增殖、生存和发展都依赖于异常的 RTK 信号传导。这些发现为旨在抑制癌症关键生物通路的靶向疗法铺平了道路。因此,RTK 已成为抗癌疗法开发的主要靶点。在过去的二十年里,许多小分子酪氨酸激酶抑制剂(TKIs)被合成并通过临床验证,目前已被有效用于治疗各种癌症类型。在本手稿中,我们旨在全面了解癌症中的 RTKs。我们探讨了不同恶性肿瘤中特定受体的各种改变和过表达,并特别关注对当前 RTK 抑制剂的研究,强调它们作为潜在靶向疗法的作用。通过整合最新的研究成果和临床证据,我们试图阐明 RTK 在癌症生物学中的关键作用,以及 RTK 抑制剂的治疗效果。
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Therapeutic advances of targeting receptor tyrosine kinases in cancer.

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.

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来源期刊
Signal Transduction and Targeted Therapy
Signal Transduction and Targeted Therapy Biochemistry, Genetics and Molecular Biology-Genetics
CiteScore
44.50
自引率
1.50%
发文量
384
审稿时长
5 weeks
期刊介绍: Signal Transduction and Targeted Therapy is an open access journal that focuses on timely publication of cutting-edge discoveries and advancements in basic science and clinical research related to signal transduction and targeted therapy. Scope: The journal covers research on major human diseases, including, but not limited to: Cancer,Cardiovascular diseases,Autoimmune diseases,Nervous system diseases.
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