colony stimulating factor 1 receptor

Nomenclature: colony stimulating factor 1 receptor

Abbreviated Name: CSFR

Family: Receptor tyrosine kinases

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 972 5q32 CSF1R colony stimulating factor 1 receptor
Mouse 1 977 18 D Csf1r colony stimulating factor 1 receptor
Rat 1 1022 18 q12.1 Csf1r colony stimulating factor 1 receptor
Previous and Unofficial Names
Colony stimulating factor 1 receptor
CD115
CSFR
C-FMS
FMS
McDonough feline sarcoma viral (v-fms) oncogene homolog
CSF-1-R
CSF-1R
M-CSF-R
MGC125014
CSF-1 receptor
fms proto-oncogene
macrophage colony-stimulating factor 1 receptor
proto-oncogene c-Fms
proto-oncogene fms
M-CSFR
Fim-2
Csfmr
c-fms
Fms
CSF1R
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
Orphanet Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  cFMS tyrosine kinase (tie2 KID) in complex with an arylamide inhibitor
PDB Id:  2I1M
Resolution:  1.8Å
Species:  Human
References:  6
Enzyme Reaction
EC Number: 2.7.10.1
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
linifanib Hs Inhibition 8.52 pIC50 1
pIC50 8.52 (IC50 3x10-9 M) [1]
dovitinib Hs Inhibition 8.52 pIC50 5
pIC50 8.52 (IC50 3x10-9 M) [5]
cediranib Hs Inhibition 6.96 pIC50 7
pIC50 6.96 (IC50 1.1x10-7 M) [7]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3,8

Key to terms and symbols Click column headers to sort
Target used in screen: CSF1R
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 9.24 pKd
PD-173955 Hs Inhibitor Inhibition 9.17 pKd
Ki-20227 Hs Inhibitor Inhibition 9.08 pKd
foretinib Hs Inhibitor Inhibition 8.74 pKd
GW-2580 Hs Inhibitor Inhibition 8.66 pKd
sunitinib Hs Inhibitor Inhibition 8.6 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.49 pKd
linifanib Hs Inhibitor Inhibition 8.47 pKd
SU-14813 Hs Inhibitor Inhibition 8.44 pKd
tandutinib Hs Inhibitor Inhibition 8.31 pKd
Target used in screen: CSF1R-autoinhibited
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 9.0 pKd
staurosporine Hs Inhibitor Inhibition 8.62 pKd
sunitinib Hs Inhibitor Inhibition 8.43 pKd
PD-173955 Hs Inhibitor Inhibition 7.85 pKd
Ki-20227 Hs Inhibitor Inhibition 7.68 pKd
GW-2580 Hs Inhibitor Inhibition 7.59 pKd
midostaurin Hs Inhibitor Inhibition 6.66 pKd
lestaurtinib Hs Inhibitor Inhibition 6.17 pKd
quizartinib Hs Inhibitor Inhibition 6.04 pKd
bosutinib Hs Inhibitor Inhibition 6.0 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: Fms/FMS
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 0.8
staurosporine Hs Inhibitor Inhibition 1.8 0.5 0.0
sorafenib Hs Inhibitor Inhibition 5.6
Cdk2 inhibitor IV Hs Inhibitor Inhibition 5.7 1.0 2.0
midostaurin Hs Inhibitor Inhibition 6.6 0.0 1.0
sunitinib Hs Inhibitor Inhibition 7.3
SU11652 Hs Inhibitor Inhibition 7.4 0.0 0.0
masitinib Hs Inhibitor Inhibition 8.4
PDGF RTK inhibitor Hs Inhibitor Inhibition 10.5 0.0 -1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 10.6 5.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Leukoencephalopathy, diffuse hereditary, with spheroids
OMIM:  221820
Orphanet:  313808
References: 
Mutations not determined

References

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1. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS et al.. (2006) Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol. Cancer Ther.5 (4): 995-1006. [PMID:16648571]

2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1039-45. [PMID:22037377]

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1046-51. [PMID:22037378]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J.451 (2): 313-28. [PMID:23398362]

5. Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M et al.. (2009) Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors. J. Med. Chem.52 (2): 278-92. [PMID:19113866]

6. Schubert C, Schalk-Hihi C, Struble GT, Ma HC, Petrounia IP, Brandt B, Deckman IC, Patch RJ, Player MR, Spurlino JC et al.. (2007) Crystal structure of the tyrosine kinase domain of colony-stimulating factor-1 receptor (cFMS) in complex with two inhibitors. J. Biol. Chem.282 (6): 4094-101. [PMID:17132624]

7. Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO et al.. (2005) AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res.65 (10): 4389-400. [PMID:15899831]

8. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol.17 (11): 1241-9. [PMID:21095574]

How to cite this page

Receptor tyrosine kinases: colony stimulating factor 1 receptor. Last modified on 13/05/2014. Accessed on 25/10/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1806.