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首页> 外文期刊>Expert opinion on therapeutic targets >Tyrosine kinases as targets in cancer therapy - successes and failures.
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Tyrosine kinases as targets in cancer therapy - successes and failures.

机译：酪氨酸激酶作为癌症治疗的靶点-成功和失败。

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Protein kinases play a crucial role in signal transduction and also in cellular proliferation, differentiation and various regulatory mechanisms. The inhibition of growth-related kinases, especially tyrosine kinases, might therefore provide new therapies for diseases such as cancer. Due to the enormous progress that has been made in the past few years in the identification of the human genome, in molecular and cell biology technologies, in structural biology and in bioinformatics, the number of receptor and non-receptor tyrosine kinases that have been identified as valuable molecular targets has greatly increased. Currently, more than 20 different tyrosine kinase targets are under evaluation in drug discovery projects in oncology. The progress made in the crystallisation of protein kinases, in most cases complexed with ATP-site-directed inhibitors, has confirmed that the ATPbinding domain of tyrosine kinases is an attractive target for rational drug design; more than 20 ATP-competitive, low molecular weight inhibitors are in various phases of clinical evaluation. Meanwhile, clinical proof-of-concept (POC) has been achieved with several antibodies and small molecules targeted against tyrosine kinases. With Herceptin, Glivec and Iressa (registered in Japan), the first kinase drugs have entered the market. This review describes the preclinical and clinical status of low molecular weight drugs targeted against different tyrosine kinases (e.g., epidermal growth factor receptor [EGFR], vascular endothelial growth factor receptor [VEGFR], platelet-derived growth factor receptor [PDGFR], Kit, Fms-like tyrosine kinase [Flt]-3), briefly describes new targets, and provides a critical analysis of the current situation in the area of tyrosine kinase inhibitors.
机译：蛋白激酶在信号转导以及细胞增殖，分化和各种调节机制中起着至关重要的作用。因此，抑制生长相关激酶，尤其是酪氨酸激酶，可能会为癌症等疾病提供新的疗法。由于过去几年在鉴定人类基因组，分子和细胞生物学技术，结构生物学和生物信息学方面取得了巨大进展，因此已确定了受体和非受体酪氨酸激酶的数量。因为有价值的分子靶标大大增加了。当前，在肿瘤学的药物发现项目中正在评估20多种不同的酪氨酸激酶靶标。在大多数情况下，与ATP定位抑制剂复合的蛋白激酶结晶方面的进展已证实，酪氨酸激酶的ATP结合域是合理药物设计的诱人靶标。在临床评估的各个阶段中，有20多种具有ATP竞争性的低分子量抑制剂。同时，已经用几种针对酪氨酸激酶的抗体和小分子实现了临床概念验证（POC）。借助赫赛汀，格列卫和易瑞沙（在日本注册），首个激酶药物已进入市场。这篇综述描述了针对不同酪氨酸激酶的低分子量药物的临床前和临床状况（例如，表皮生长因子受体[EGFR]，血管内皮生长因子受体[VEGFR]，血小板源性生长因子受体[PDGFR]，试剂盒， Fms样酪氨酸激酶[Flt] -3）简要描述了新的靶标，并对酪氨酸激酶抑制剂领域的现状提供了重要的分析。

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