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c-Kit受体作为癌症治疗靶点的当前见解

c-Kit Receptors as a Therapeutic Target in Cancer: Current Insights.

作者信息

Abdellateif Mona S, Bayoumi Ahmed K, Mohammed Mohammed Aly

机构信息

Medical Biochemistry and Molecular Biology, Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, 11796, Egypt.

Paediatric Oncology Department, National Cancer Institute, Cairo University, Cairo, 11796, Egypt.

出版信息

Onco Targets Ther. 2023 Sep 27;16:785-799. doi: 10.2147/OTT.S404648. eCollection 2023.

Abstract

c-Kit is a type III receptor tyrosine kinase (RTK) that has an essential role in various biological functions including gametogenesis, melanogenesis, hematopoiesis, cell survival, and apoptosis. c-KIT aberrations, either overexpression or loss-of-function mutations, have been implicated in the pathogenesis and development of many cancers, including gastrointestinal stromal tumors, mastocytosis, acute myeloid leukemia, breast, thyroid, and colorectal cancer, making c-KIT an attractive molecular target for the treatment of cancers. Therefore, a lot of effort has been put into investigating the utility of tyrosine kinase inhibitors for the management of c-KIT mutated tumors. This review of the literature illustrates the role of c-KIT mutations in many cancers, aiming to provide insights into the role of TKIs as a therapeutic option for cancer patients with c-KIT aberrations. In conclusion, c-KIT is implicated in different types of cancer, and it could be a successful molecular target; however, proper detection of the underlying mutation type is required before starting the appropriate personalized therapy.

摘要

c-Kit是一种III型受体酪氨酸激酶(RTK),在多种生物学功能中发挥着重要作用,包括配子发生、黑色素生成、造血作用、细胞存活和细胞凋亡。c-KIT异常,无论是过表达还是功能丧失突变,都与许多癌症的发病机制和发展有关,包括胃肠道间质瘤、肥大细胞增多症、急性髓系白血病、乳腺癌、甲状腺癌和结直肠癌,这使得c-KIT成为治疗癌症的一个有吸引力的分子靶点。因此,人们投入了大量精力来研究酪氨酸激酶抑制剂在治疗c-KIT突变肿瘤方面的效用。这篇文献综述阐述了c-KIT突变在许多癌症中的作用,旨在深入了解酪氨酸激酶抑制剂作为c-KIT异常癌症患者治疗选择的作用。总之,c-KIT与不同类型的癌症有关,它可能是一个成功的分子靶点;然而,在开始适当的个性化治疗之前,需要正确检测潜在的突变类型。

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