FLT3 tyrosine kinase inhibitors
FLT3 tyrosine kinase inhibitors
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DOI：
10.1532/ijh97.05079
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发表时间：
2005-08-01
影响因子：
2.1
通讯作者：
Small, D
中科院分区：
文献类型：
--
作者：
Levis, M;Small, D
受体酪氨酸激酶FLT3是造血过程中重要的调控分子，在大多数急性白血病的原始细胞上表达。这种受体的激活突变存在于大约30%的急性髓性白血病（AML）患者中，并与明显更差的临床结局相关。针对该突变并改善该AML患者亚组的结局的努力导致了对几种新型小分子FLT3酪氨酸激酶抑制剂的研究。这些化合物来源于各种各样的化学类别，并且在效力和选择性方面存在显著差异。在这篇综述中，我们讨论了FLT3抑制剂的临床前，临床和相关实验室研究的结果，以证明这一领域是如何代表一个真正的翻译企业与实验室和临床之间的多个正在进行的相互作用。
The receptor tyrosine kinase FLT3 is an important regulatory molecule in hematopoiesis and is expressed on the blasts in most cases of acute leukemia. Activating mutations of this receptor are present in roughly 30% of acute myeloid leukemia (AML) patients and are associated with a distinctly worse clinical outcome. Efforts to target this mutation and improve outcomes in this subgroup of AML patients have led to the investigation of several novel small-molecule FLT3 tyrosine kinase inhibitors. These compounds derive from a wide variety of chemical classes and differ significantly, both in their potency and in their selectivity. In this review, we discuss the results of preclinical, clinical, and correlative laboratory studies of FLT3 inhibitors in demonstrating how this field represents a truly translational enterprise with multiple ongoing interactions between the laboratory and the clinic.