Mast Cell Biology Section, Laboratory of Allergic Diseases, National Institute of Allergy and Infectious Diseases (NIAID), National Institutes of Health, 10 Center Drive, Building 10, Room 11C207, MSC 1881, Bethesda, MD 20892, USA.
Mast Cell Biology Section, Laboratory of Allergic Diseases, National Institute of Allergy and Infectious Diseases (NIAID), National Institutes of Health, 10 Center Drive, Building 10, Room 11C207, MSC 1881, Bethesda, MD 20892, USA.
Immunol Allergy Clin North Am. 2014 May;34(2):219-37. doi: 10.1016/j.iac.2014.01.002. Epub 2014 Mar 12.
In this review, the authors discuss common gain-of-function mutations in the stem cell factor receptor KIT found in mast cell proliferation disorders and summarize the current understanding of the molecular mechanisms by which these transforming mutations may affect KIT structure and function leading to altered downstream signaling and cellular transformation. Drugs targeting KIT have shown mixed success in the treatment of mastocytosis and other hyperproliferative diseases. A brief overview of the most common KIT inhibitors currently used, the reasons for the varied clinical results of such inhibitors and a discussion of potential new strategies are provided.
在这篇综述中，作者讨论了干细胞因子受体 KIT 中的常见功能获得性突变，这些突变存在于肥大细胞增殖障碍中，并总结了目前对这些转化突变如何影响 KIT 结构和功能，从而导致下游信号转导和细胞转化改变的分子机制的理解。针对 KIT 的药物在肥大细胞瘤和其他增殖性疾病的治疗中取得了喜忧参半的效果。本文简要概述了目前最常用的 KIT 抑制剂，讨论了此类抑制剂临床疗效差异的原因，并探讨了潜在的新策略。
