Tyrosine Kinase Inhibitors for Pediatric Leukemia: History and Current Status.

IF 2.1 4区 医学 Q3 MEDICINE, RESEARCH & EXPERIMENTAL
Discovery medicine Pub Date : 2022-03-01
Li-Rong Sun, Ling-Zhen Wang, Ren Zhong, Yan-Xia Zhao, Yan Sun
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引用次数: 0

Abstract

Tyrosine kinase inhibitors (TKIs) block the activity of tyrosine kinases by competitive inhibition of ATP at the catalytic tyrosine kinase binding site and inhibit oncogenic signaling. One important target of TKIs is BCR-ABL1, which is constitutively activated in leukemia cells. In this review, we briefly describe the development of TKIs from the first generation to the third generation, and summarize their use in the treatment of chronic myeloid leukemia and acute lymphoblastic leukemia in children. We highlight several future directions in the development of TKIs for pediatric leukemia therapy. In conclusion, we focus on chronic myeloid leukemia and acute lymphoblastic leukemia as the examples of pediatric blood cancer that significantly benefit from TKIs-based target therapy. Further development of TKIs will allow us to better manage pediatric leukemia.

酪氨酸激酶抑制剂治疗儿童白血病:历史和现状。
酪氨酸激酶抑制剂(TKIs)通过竞争性抑制酪氨酸激酶结合位点的ATP来阻断酪氨酸激酶的活性,并抑制致癌信号传导。TKIs的一个重要靶点是BCR-ABL1,它在白血病细胞中被组成性激活。在本文中,我们简要介绍了TKIs从第一代到第三代的发展,并总结了它们在治疗儿童慢性髓性白血病和急性淋巴细胞白血病中的应用。我们强调了TKIs用于儿科白血病治疗的几个未来发展方向。总之,我们将重点放在慢性髓系白血病和急性淋巴细胞白血病作为儿童血癌的例子,这些例子明显受益于基于tkis的靶向治疗。tki的进一步发展将使我们能够更好地管理儿童白血病。
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来源期刊
Discovery medicine
Discovery medicine MEDICINE, RESEARCH & EXPERIMENTAL-
CiteScore
5.40
自引率
0.00%
发文量
80
审稿时长
6-12 weeks
期刊介绍: Discovery Medicine publishes novel, provocative ideas and research findings that challenge conventional notions about disease mechanisms, diagnosis, treatment, or any of the life sciences subjects. It publishes cutting-edge, reliable, and authoritative information in all branches of life sciences but primarily in the following areas: Novel therapies and diagnostics (approved or experimental); innovative ideas, research technologies, and translational research that will give rise to the next generation of new drugs and therapies; breakthrough understanding of mechanism of disease, biology, and physiology; and commercialization of biomedical discoveries pertaining to the development of new drugs, therapies, medical devices, and research technology.
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