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. 2017 Oct 21;174(Suppl Suppl 1):S225–S271. doi: 10.1111/bph.13876
Nomenclature colony stimulating factor 1 receptor fms related tyrosine kinase 3
HGNC, UniProt CSF1R, P07333 FLT3, P36888
EC number 2.7.10.1 2.7.10.1
Common abreviation CSFR FLT3
Endogenous ligands G‐CSF (CSF3, P09919), GM‐CSF (CSF2, P04141), M‐CSF (CSF1, P09603) Fms‐related tyrosine kinase 3 ligand (FLT3LG, P49771)
Inhibitors JNJ‐28312141 (pIC50 9.2) [116], Ki‐20227 (pK d 9.1) [33], Ki‐20227 (pIC50 8.7) [143], GW‐2580 (pK d 8.7) [33], JNJ‐28312141 (pK d 8.5) [33] AC710 (pK d 9.3) [108], linifanib (pK d 9.2) [33], dovitinib (pK d 9.2) [33], crenolanib (pK d 9.1) [69], AST‐487 (pK d 9.1) [33], ENMD‐2076 (pIC50 8.5) [149], tandutinib (pK d 8.5) [33]
Selective inhibitors GW‐2580 (pIC50 7.2) [27] G749 (pIC50 9.4) [97]
Comments Upregulation of CSF1R expression is associated with migroglial activation and immune pathology in Alzhermer's disease (AD) [67, 61]. Pharmacological inhibition of CSF1R with GW‐2580 reduces microglial proliferation and prevents disease progression in a mouse model of AD, but this does not correlate with amyloid‐β plaque numbers [144]. 5'‐fluoroindirubinoxime has been described as a selective FLT3 inhibitor [22].