CSF-1R
CSF1R (Colony stimulating factor 1 receptor,M-CSFR,CD115) is a receptor for a cytokine called colony stimulating factor 1. It controls the production, differentiation, and function of macrophages. This receptor mediates most, if not all, of the biological effects of this cytokine. Ligand binding activates CSF1R through a process of oligomerization and trans-phosphorylation. The encoded protein is a tyrosine kinase transmembrane receptor and member of the CSF1/PDGF receptor family of tyrosine-protein kinases.
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GW2580是c-FMS激酶口服活性抑制剂,体外实验60nM浓度能完全抑制c-FMS酶活性,对其他26种激酶没有抑制作用。
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BLZ945是CSF1R高效选择性抑制剂,IC50值为1 nM,对其他激酶基本无作用。
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Pexidartinib是受体酪氨酸激酶Fms,Kit和Flt3小分子抑制剂,临床2期。
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