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小分子靶向c-Fms抑制剂的研究进展

Progress in Small-Molecular Inhibitors Targeting c-Fms
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摘要 巨噬细胞集落刺激因子受体(c-Fms)是原癌基因fms编码的产物,为Ⅲ型酪氨酸激酶。c-Fms及其配体CSF-1在肿瘤相关巨噬细胞的增殖、生长、分化过程中起着重要作用。c-Fms在多种恶性肿瘤和炎性疾病中异常表达,CSF-1/c-Fms轴可能成为治疗恶性肿瘤的有效途径。许多以c-Fms为靶标的小分子抑制剂正在研究与临床开发中。简介c-Fms的结构特征和作用机制,对小分子靶向c-Fms抑制剂的研究进展进行综述,以期为相关研究提供参考。 Macrophage colony stimulating factor receptor (c-Fms), the product encoded by proto-oncogene fins, is a type III receptor tyrosme kinase, c-Fins and its ligand CSF-1 play important roles in the proliferation, growth and differentiation of tumor-associated macrophages. c-Fms is abnormally expressed in a variety of malignant and inflammatory diseases. The CSF-I/c-Fms axis might be an effective approach to the treatment of malignant tumors, Many small molecular inhibitors targeting c-Fins are under research and clinical development. This article describes the mechanisms of c-Fms and its roles in tumor immunotherapy, and reviews the latest research progress in small-molecule inhibitors of c-Fins, so as to provide reference for follow-up studies.
作者 王凯成 张方青 杨晓骏 张惠斌 周金培 WANG Kaicheng;ZHANG Fangqing;YANG Xiaojun;ZHANG Huibin;ZHOU Jinpei(Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China)
出处 《药学进展》 CAS 2018年第7期517-526,共10页 Progress in Pharmaceutical Sciences
关键词 c-Fms抑制剂 抗肿瘤 巨噬细胞集落刺激因子 肿瘤相关巨噬细胞 c-Fms inhibitor anti-cancer macrophage colony stimulating factor tumor-associated macrophage
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