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Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2018-01-02 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00873
Mohammed I. El-Gamal 1, 2 , Shahad K. Al-Ameen 1 , Dania M. Al-Koumi 1 , Mawadda G. Hamad 1 , Nouran A. Jalal 1 , Chang-Hyun Oh 3, 4
Affiliation  

Colony stimulation factor-1 receptor (CSF-1R), which is also known as FMS kinase, plays an important role in initiating inflammatory, cancer, and bone disorders when it is overstimulated by its ligand, CSF-1. Innate immunity, as well as macrophage differentiation and survival, are regulated by the stimulation of the CSF-1R. Another ligand, interlukin-34 (IL-34), was recently reported to activate the CSF-1R receptor in a different manner. The relationship between CSF-1R and microglia has been reviewed. Both CSF-1 antibodies and small molecule CSF-1R kinase inhibitors have now been tested in animal models and in humans. In this Perspective, we discuss the role of CSF-1 and IL-34 in producing cancer, bone disorders, and inflammation. We also review the newly discovered and improved small molecule kinase inhibitors and monoclonal antibodies that have shown potent activity toward CSF-1R, reported from 2012 until 2017.

中文翻译:

集落刺激因子1受体(CSF-1R)激酶及其抑制剂的最新研究进展

当其配体CSF-1过度刺激时,菌落刺激因子1受体(CSF-1R)也称为FMS激酶,在引发炎症,癌症和骨骼疾病中起重要作用。先天免疫以及巨噬细胞的分化和存活都受到CSF-1R刺激的调节。最近报道了另一种配体白细胞介素34(IL-34)以不同的方式激活CSF-1R受体。CSF-1R和小胶质细胞之间的关系进行了审查。现在已经在动物模型和人类中测试了CSF-1抗体和小分子CSF-1R激酶抑制剂。在此观点中,我们讨论了CSF-1和IL-34在产生癌症,骨骼疾病和炎症中的作用。
更新日期:2018-01-02
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