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colony stimulating factor 1 receptor

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1806

Nomenclature: colony stimulating factor 1 receptor

Abbreviated Name: CSFR

Family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 972 5q32 CSF1R colony stimulating factor 1 receptor
Mouse 1 977 18 34.41 cM Csf1r colony stimulating factor 1 receptor
Rat 1 978 18q12.1 Csf1r colony stimulating factor 1 receptor
Previous and Unofficial Names Click here for help
CD115 | C-FMS | CSF-1 receptor | Csfmr | Fim-2 | macrophage colony-stimulating factor 1 receptor | McDonough feline sarcoma viral (v-fms) oncogene homolog | M-CSFR
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
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:  32
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of FMS KINASE domain with a small molecular inhibitor, PLX3397.
PDB Id:  4R7H
Ligand:  pexidartinib
Resolution:  2.8Å
Species:  Human
References:  35
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
G-CSF {Sp: Human}
GM-CSF {Sp: Human}
IL-34 {Sp: Human}
M-CSF {Sp: Human}

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Ki-20227 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.1 pKd 12
pKd 9.1 (Kd 8.3x10-10 M) [12]
IACS-9439 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pKd 11
pKd 9.0 (Kd 1x10-9 M) [11]
AC710 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pKd 26
pKd 8.8 (Kd 1.57x10-9 M) [26]
GW-2580 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKd 12
pKd 8.7 (Kd 2.2x10-9 M) [12]
JNJ-28312141 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pKd 12
pKd 8.5 (Kd 3.2x10-9 M) [12]
BLZ945 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pKd 11
pKd 8.5 (Kd 3.4x10-9 M) [11]
quizartinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pKd 7
pKd 7.9 (Kd 1.2x10-8 M) [7]
crenolanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.5 pKd 22
pKd 7.5 (Kd 3x10-8 M) [22]
JNJ-28312141 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.2 pIC50 27
pIC50 9.2 (IC50 6.9x10-10 M) [27]
compound 29 [PMID: 31934767] Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 41
pIC50 9.1 (IC50 7x10-10 M) [41]
Description: Determined in an ELISA assay detecting tyrosine phosphorylation using immobilised recombinant CSF-1R protein.
BLZ945 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.0 pIC50 34
pIC50 9.0 (IC50 1x10-9 M) [34]
IACS-9439 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pIC50 11
pIC50 8.8 (IC50 1.7x10-9 M) [11]
Ki-20227 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 30
pIC50 8.7 (IC50 2x10-9 M) [30]
GR-389988 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.7 pIC50 23
pIC50 8.7 (IC50 2x10-9 M) [23]
Description: In a biochemical assay measuring inhibition of peptide substrate phosphorylation by the test compound in the presence ot recombinant human c-FMS.
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3x10-9 M) [3]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 19
pIC50 8.5 (IC50 3x10-9 M) [19]
Description: Measuring inhibition of kinase activity in a biochemical assay.
edicotinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.5 pIC50 18
pIC50 8.5 (IC50 3.2x10-9 M) [18]
cerdulatinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 8
pIC50 8.3 (IC50 5x10-9 M) [8]
AZD6495 Small molecule or natural product Primary target of this compound Hs Inhibition 8.2 pIC50 33
pIC50 8.2 (IC50 6x10-9 M) [33]
CS2164 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 42
pIC50 8.1 (IC50 7x10-9 M) [42]
ARRY-382 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 8.1 pIC50 5
pIC50 8.1 (IC50 9x10-9 M) [5]
vimseltinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition >8.0 pIC50 2
pIC50 >8.0 (IC50 <1x10-8 M) [2]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 – 8.5 pIC50 31,36
pIC50 7.4 – 8.5 (IC50 3.6x10-8 – 3x10-9 M) [31,36]
pexidartinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 35
pIC50 7.9 (IC50 1.3x10-8 M) [35]
OSI-930 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 17
pIC50 7.8 (IC50 1.5x10-8 M) [17]
CHMFL-KIT-64 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 40
pIC50 7.7 (IC50 1.8x10-8 M) [40]
Description: In a biochemical assay.
zotiraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 20
pIC50 7.6 (IC50 2.7x10-8 M) [20]
CC-223 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 28
pIC50 7.6 (IC50 2.8x10-8 M) [28]
GW-2580 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 9
pIC50 7.2 (IC50 6x10-8 M) [9]
cediranib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 37
pIC50 7.0 (IC50 1.1x10-7 M) [37]
pazopanib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.8 pIC50 21
pIC50 6.8 (IC50 1.46x10-7 M) [21]
GTP-14564 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.5 pIC50 29
pIC50 6.5 (IC50 3x10-7 M) [29]
tandutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.5 pIC50 24
pIC50 5.5 (IC50 3.43x10-6 M) [24]
Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
IL-34 {Sp: Human} Peptide Immunopharmacology Ligand Hs Agonist - - 25
[25]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
emactuzumab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 9.5 pKd 13
pKd 9.5 (Kd 2.9x10-10 M) [13]
Description: Affinity data measured by surface plasmon resonance.
AMG820 Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding >9.3 pKd 6
pKd >9.3 (Kd <5.5x10-10 M) [6]
cabiralizumab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding >9.0 pKd 39
pKd >9.0 (Kd <1x10-9 M) [39]
LY3022855 Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 10.1 pEC50 14
pEC50 10.1 (EC50 9x10-11 M) [14]
Description: Measured in an ELISA binding assay.
DiscoveRx KINOMEscan® screen Click here for help
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: 12,38

Key to terms and symbols Click column headers to sort
Target used in screen: CSF1R
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
GW-2580 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 8.4 pKd
tandutinib Small molecule or natural product Hs Inhibitor Inhibition 8.3 pKd
Target used in screen: CSF1R-autoinhibited
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
GW-2580 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
quizartinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 Click here for help
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: 4,16

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 Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 0.8
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.8 0.5 0.0
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.6
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 1.0 2.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 0.0 1.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 0.0 0.0
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.4
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 10.5 0.0 -1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.6 5.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
Activation of the CSF1R induces myeloid proliferation, and in the tumour microenvironment this promotes M1 to M2 polarization and accumulation of tumour-associated macrophages (TAMs). The CSF1R is therefore being investigated as an immuno-oncology drug target [1]. It is the primary target of several in development tyrosine kinase inhibitors such as pexidartinib, GW-2580 and BLZ945, and the investigational monoclonal antibodies AMG820, LY3022855 and cabiralizumab (FPA-008).
Cell Type Associations
Immuno Cell Type:  Other T cells
Comment:  Expression down-regulated in response to HMB-PP or OKT-3 activation
References:  10
Immuno Cell Type:  Natural killer cells
Comment:  Down-regulated expression measured by Affymetrix GeneChip array, in experiments designed to expand NK cell populations as a potential cancer immunotherapy tool.
References:  15
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0006954 inflammatory response TAS
GO:0010759 positive regulation of macrophage chemotaxis IGI
click arrow to show/hide IEA associations
GO:0045087 innate immune response IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 6 GO processes
GO:0002244 hematopoietic progenitor cell differentiation IBA
GO:0030097 hemopoiesis IMP
GO:0030224 monocyte differentiation TAS
GO:0030225 macrophage differentiation TAS
GO:0030316 osteoclast differentiation ISS
GO:0045672 positive regulation of osteoclast differentiation ISO
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 6 GO processes
GO:0005011 macrophage colony-stimulating factor receptor activity IMP
GO:0019221 cytokine-mediated signaling pathway IMP
GO:0032722 positive regulation of chemokine production IMP
GO:0036006 cellular response to macrophage colony-stimulating factor stimulus IMP
GO:0038145 macrophage colony-stimulating factor signaling pathway ISS
GO:0071345 cellular response to cytokine stimulus ISS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 2 GO processes
GO:0010759 positive regulation of macrophage chemotaxis IGI
GO:0032722 positive regulation of chemokine production IMP
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes
GO:0010759 positive regulation of macrophage chemotaxis IGI
GO:0045672 positive regulation of osteoclast differentiation ISO
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Leukoencephalopathy, diffuse hereditary, with spheroids
Synonyms: Hereditary diffuse leukoencephalopathy with axonal spheroids and pigmented glia [Orphanet: ORPHA313808]
OMIM: 221820
Orphanet: ORPHA313808

References

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1. Adams JL, Smothers J, Srinivasan R, Hoos A. (2015) Big opportunities for small molecules in immuno-oncology. Nat Rev Drug Discov, 14 (9): 603-22. [PMID:26228631]

2. Ahn Y,Vogeti L, Caldwell TM, Kaufman MD, Flynn DL. (2014) 2-aminopyrimidin-6-ones and analogs exhibiting anti-cancer and anti-proliferative activities. Patent number: WO2014145025A2. Assignee: Deciphera Pharmaceuticals, Llc. Priority date: 15/03/2013. Publication date: 18/09/2014.

3. 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]

4. 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]

5. Bendell J et al.. A Phase 1 Study of ARRY-382, an Oral Inhibitor of Colony-stimulating Factor-1 Receptor (CSF1R), in Patients with Advanced or Metastatic Cancers. Accessed on 14/04/2016. Modified on 14/04/2016. Arraybiopharma.com, http://www.arraybiopharma.com/files/3014/4501/8593/382-101_AACR-NCI-EORTC_poster.pdf

6. Brasel KA, Foster S, Cerretti DP, Sun J, Smothers JF, Mehlin C. (2009) Human c-fms antigen binding proteins. Patent number: WO2009026303 A1. Assignee: Amgen Inc.. Priority date: 21/08/2007. Publication date: 26/02/2009.

7. Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, Gunawardane RN, Cramer MD, Gardner MF, James J et al.. (2009) Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. J Med Chem, 52 (23): 7808-16. [PMID:19754199]

8. Coffey G, Betz A, DeGuzman F, Pak Y, Inagaki M, Baker DC, Hollenbach SJ, Pandey A, Sinha U. (2014) The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther, 351 (3): 538-48. [PMID:25253883]

9. Conway JG, McDonald B, Parham J, Keith B, Rusnak DW, Shaw E, Jansen M, Lin P, Payne A, Crosby RM et al.. (2005) Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci USA, 102 (44): 16078-83. [PMID:16249345]

10. Correia DV, d'Orey F, Cardoso BA, Lança T, Grosso AR, deBarros A, Martins LR, Barata JT, Silva-Santos B. (2009) Highly active microbial phosphoantigen induces rapid yet sustained MEK/Erk- and PI-3K/Akt-mediated signal transduction in anti-tumor human gammadelta T-cells. PLoS ONE, 4 (5): e5657. [PMID:19479075]

11. Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E et al.. (2020) Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R. J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.0c00936 [PMID:32787110]

12. 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]

13. Dimoudis N, Fertig G, Fidler A, Pickl M, Ries C, Seeber S, Lanzendoerfer M, Krueger K. (2011) Antibodies against human csf-1r and uses thereof. Patent number: US20110165156 A1. Assignee: Dimoudis N, Fertig G, Fidler A, Pickl M, Ries C, Seeber S, Lanzendoerfer M, Krueger K.. Priority date: 10/12/2009. Publication date: 07/07/2011.

14. Doody JF, Li Y. (2011) Antibodies against csf-1r. Patent number: WO2011123381 A1. Assignee: Imclone Llc. Priority date: 01/04/2010. Publication date: 06/10/2011.

15. Fujisaki H, Kakuda H, Shimasaki N, Imai C, Ma J, Lockey T, Eldridge P, Leung WH, Campana D. (2009) Expansion of highly cytotoxic human natural killer cells for cancer cell therapy. Cancer Res, 69 (9): 4010-7. [PMID:19383914]

16. 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]

17. Garton AJ, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN et al.. (2006) OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res, 66 (2): 1015-24. [PMID:16424037]

18. Genovese MC, Hsia E, Belkowski SM, Chien C, Masterson T, Thurmond RL, Manthey CL, Yan XD, Ge T, Franks C et al.. (2015) Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy. J Rheumatol, 42 (10): 1752-60. [PMID:26233509]

19. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al.. (2012) Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther, 343 (3): 617-27. [PMID:22935731]

20. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia, 26 (2): 236-43. [PMID:21860433]

21. Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter 3rd RN, Johnson JH et al.. (2008) Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem, 51 (15): 4632-40. [PMID:18620382]

22. Heinrich MC, Griffith D, McKinley A, Patterson J, Presnell A, Ramachandran A, Debiec-Rychter M. (2012) Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res, 18 (16): 4375-84. [PMID:22745105]

23. Kane JL Jr, Matthews G, Metz M, Kothe M, Liu J, Scholte A. (2015) Tropomyosin-related kinase (Trk) inhibitors. Patent number: US9174986B2. Assignee: Genzyme Corp.. Priority date: 10/12/2013. Publication date: 03/11/2015.

24. Kelly LM, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM, Williams I, Amaral SM, Curley DP, Duclos N et al.. (2002) CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell, 1 (5): 421-32. [PMID:12124172]

25. Lin H, Lee E, Hestir K, Leo C, Huang M, Bosch E, Halenbeck R, Wu G, Zhou A, Behrens D et al.. (2008) Discovery of a cytokine and its receptor by functional screening of the extracellular proteome. Science, 320 (5877): 807-11. [PMID:18467591]

26. Liu G, Campbell BT, Holladay MW, Ford Pulido JM, Hua H, Gitnick D, Gardner MF, James J, Breider MA, Brigham D et al.. (2012) Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases. ACS Med Chem Lett, 3 (12): 997-1002. [PMID:24900421]

27. Manthey CL, Johnson DL, Illig CR, Tuman RW, Zhou Z, Baker JF, Chaikin MA, Donatelli RR, Franks CF, Zeng L et al.. (2009) JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia. Mol Cancer Ther, 8 (11): 3151-61. [PMID:19887542]

28. Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG et al.. (2015) Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. J Med Chem, 58 (13): 5323-33. [PMID:26083478]

29. Murata K, Kumagai H, Kawashima T, Tamitsu K, Irie M, Nakajima H, Suzu S, Shibuya M, Kamihira S, Nosaka T et al.. (2003) Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3). J Biol Chem, 278 (35): 32892-8. [PMID:12815052]

30. Ohno H, Kubo K, Murooka H, Kobayashi Y, Nishitoba T, Shibuya M, Yoneda T, Isoe T. (2006) A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther, 5 (11): 2634-43. [PMID:17121910]

31. 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]

32. 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]

33. Scott DA, Bell KJ, Campbell CT, Cook DJ, Dakin LA, Del Valle DJ, Drew L, Gero TW, Hattersley MM, Omer CA et al.. (2009) 3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile. Bioorg Med Chem Lett, 19 (3): 701-5. [PMID:19114305]

34. Strachan DC, Ruffell B, Oei Y, Bissell MJ, Coussens LM, Pryer N, Daniel D. (2013) CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8(+) T cells. Oncoimmunology, 2 (12): e26968. [PMID:24498562]

35. Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI et al.. (2015) Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N Engl J Med, 373 (5): 428-37. [PMID:26222558]

36. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK. (2005) CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood, 105 (7): 2941-8. [PMID:15598814]

37. 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]

38. 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]

39. Wong J, Vasquez M. (2011) Antibodies That Bind CSF1R. Patent number: US20110274683 A1. Assignee: Five Prime Therapeutics, Inc.. Priority date: 04/05/2010. Publication date: 10/11/2011.

40. Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C et al.. (2019) Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. J Med Chem, 62 (13): 6083-6101. [PMID:31250638]

41. Xie Z, Wu B, Liu Y, Ren W, Tong L, Xiang C, Wei A, Gao Y, Zeng L, Xie H et al.. (2020) Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an o-Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders. J Med Chem, 63 (3): 1397-1414. [PMID:31934767]

42. Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao JZ et al.. (2017) CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci, 108 (3): 469-477. [PMID:28004478]

How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: colony stimulating factor 1 receptor. Last modified on 19/08/2020. Accessed on 20/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1806.