Receptor tyrosine kinase (c-Kit) inhibitors: a potential therapeutic target in cancer cells.
Receptor tyrosine kinase (c-Kit) inhibitors: a potential therapeutic target in cancer cells.
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DOI：
10.2147/dddt.s89114
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Ahmadipour F
中科院分区：
文献类型：
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作者：
Abbaspour Babaei M;Kamalidehghan B;Saleem M;Huri HZ;Ahmadipour F
c-Kit是一种受体酪氨酸激酶，参与细胞内信号传导，并且c-Kit的突变形式在一些癌症的发生中起关键作用。c-Kit的功能导致了抑制c-Kit激酶活性可以成为癌症治疗的靶点的概念。在胃肠道间质瘤、急性髓性白血病、黑色素瘤等癌症中，已经观察到抑制c-Kit治疗癌症的有希望的结果，这些结果促使人们尝试改进使用c-Kit作为癌症治疗的有效靶点。本文介绍了c-Kit作为受体酪氨酸激酶和癌基因的研究结果，以及其在正常细胞和癌细胞中的基因靶点和信号通路。本文对c-Kit的基因定位、蛋白结构及其在正常细胞中的作用进行了讨论。因此，理解c-Kit介导的肿瘤发生的分子机制是至关重要的，并可能导致未来新的药物靶点的鉴定。已经描述了c-Kit诱导细胞转化的潜在机制。本研究旨在阐明c-Kit在未来癌症治疗中的作用。此外，它具有c-Kit抑制剂药物特性，其功能已在表格中列出并在示意图中展示。这篇综述还收集了以前的研究，靶向c-Kit作为一种新的癌症治疗策略。本文进一步强调了这种方法的优点，以及在未来必须解决的局限性。最后，尽管c-Kit是癌症治疗的一个有吸引力的靶点，但根据c-Kit抑制剂治疗患者的结果，单独使用Kit抑制剂不太可能治愈。似乎单独的c-Kit突变不足以促进肿瘤发生，但确实在癌症发生中起着至关重要的作用。
c-Kit, a receptor tyrosine kinase, is involved in intracellular signaling, and the mutated form of c-Kit plays a crucial role in occurrence of some cancers. The function of c-Kit has led to the concept that inhibiting c-Kit kinase activity can be a target for cancer therapy. The promising results of inhibition of c-Kit for treatment of cancers have been observed in some cancers such as gastrointestinal stromal tumor, acute myeloid leukemia, melanoma, and other tumors, and these results have encouraged attempts toward improvement of using c-Kit as a capable target for cancer therapy. This paper presents the findings of previous studies regarding c-Kit as a receptor tyrosine kinase and an oncogene, as well as its gene targets and signaling pathways in normal and cancer cells. The c-Kit gene location, protein structure, and the role of c-Kit in normal cell have been discussed. Comprehending the molecular mechanism underlying c-Kit-mediated tumorogenesis is consequently essential and may lead to the identification of future novel drug targets. The potential mechanisms by which c-Kit induces cellular transformation have been described. This study aims to elucidate the function of c-Kit for future cancer therapy. In addition, it has c-Kit inhibitor drug properties and their functions have been listed in tables and demonstrated in schematic pictures. This review also has collected previous studies that targeted c-Kit as a novel strategy for cancer therapy. This paper further emphasizes the advantages of this approach, as well as the limitations that must be addressed in the future. Finally, although c-Kit is an attractive target for cancer therapy, based on the outcomes of treatment of patients with c-Kit inhibitors, it is unlikely that Kit inhibitors alone can lead to cure. It seems that c-Kit mutations alone are not sufficient for tumorogenesis, but do play a crucial role in cancer occurrence.