FER tyrosine kinase | Fer family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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FER tyrosine kinase

  Target has curated data in GtoImmuPdb

Target id: 2022

Nomenclature: FER tyrosine kinase

Abbreviated Name: Fer

Family: Fer family

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 - 822 5q21 FER FER tyrosine kinase
Mouse - 823 17 E1.1 Fer fer (fms/fps related) protein kinase
Rat - 453 9 q37 Fer FER tyrosine kinase
Previous and Unofficial Names
c-FER | PPP1R74 | protein phosphatase 1, regulatory subunit 74 | TYK3 | tyrosine protein kinase FLK | fer (fms/fps related) protein kinase, testis specific 2 | fer (fps/fes related) tyrosine kinase
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution structure of sh2 domain of proto-oncogene tyrosine-protein kinase fer from homo sapiens, northeast structural genomics consortium (nesg) target hr3461d
PDB Id:  2KK6
Resolution:  0.0Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.10.2

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
Ro3280 Hs Inhibition 7.3 pKd 2
pKd 7.3 (Kd 5.3x10-8 M) [2]
Description: Ambit selectivity screen at 1μM Ro3280.
compound 8e [PMID: 24432909] Hs Inhibition 8.7 pIC50 6
pIC50 8.7 (IC50 2x10-9 M) [6]
compound 25b [PMID: 22564207] Hs Inhibition 7.1 pIC50 5
pIC50 7.1 (IC50 8.5x10-8 M) [5]
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: 3,7

Key to terms and symbols Click column headers to sort
Target used in screen: FER
Ligand Sp. Type Action Affinity Parameter
NVP-TAE684 Hs Inhibitor Inhibition 8.9 pKd
GSK-1838705A Hs Inhibitor Inhibition 8.0 pKd
staurosporine Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Hs Inhibitor Inhibition 7.6 pKd
SU-14813 Hs Inhibitor Inhibition 7.5 pKd
foretinib Hs Inhibitor Inhibition 7.4 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.9 pKd
tamatinib Hs Inhibitor Inhibition 6.9 pKd
crizotinib Hs Inhibitor Inhibition 6.6 pKd
bosutinib Hs Inhibitor Inhibition 6.4 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: Fer/FER
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.8 2.0 0.5
K-252a Hs Inhibitor Inhibition 1.8 2.0 0.0
SB 218078 Hs Inhibitor Inhibition 5.4 33.0 20.0
Gö 6976 Hs Inhibitor Inhibition 5.9 4.0 4.0
SU11652 Hs Inhibitor Inhibition 17.7 79.0 14.0
Syk inhibitor Hs Inhibitor Inhibition 20.0 35.0 9.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 21.7 23.0 1.0
midostaurin Hs Inhibitor Inhibition 22.4 26.0 14.0
indirubin derivative E804 Hs Inhibitor Inhibition 28.8 37.0 35.0
sunitinib Hs Inhibitor Inhibition 31.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
FER acts downstream of the activated high affinity immunoglobulin epsilon receptor (FCεR1) and plays a role in FCεR1-mediated signaling in mast cells, regulation of mast cell degranulation, leukocyte recruitment, and leukocyte extravasation following bacterial lipopolysaccharide (LPS) exposure.
Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 4 GO processes
GO:0033007 negative regulation of mast cell activation involved in immune response ISS
GO:0043304 regulation of mast cell degranulation IBA
GO:0045087 innate immune response IBA
GO:0050904 diapedesis ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0033007 negative regulation of mast cell activation involved in immune response ISS
GO:0038095 Fc-epsilon receptor signaling pathway ISS
GO:0043304 regulation of mast cell degranulation IBA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 4 GO processes
GO:0019221 cytokine-mediated signaling pathway IMP
GO:0036006 cellular response to macrophage colony-stimulating factor stimulus IMP
GO:0038109 Kit signaling pathway ISS
GO:0070102 interleukin-6-mediated signaling pathway IMP
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0050904 diapedesis ISS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0033007 negative regulation of mast cell activation involved in immune response ISS
GO:0038095 Fc-epsilon receptor signaling pathway ISS
GO:0043304 regulation of mast cell degranulation IBA

References

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1. 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]

2. Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S et al.. (2012) Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg. Med. Chem. Lett., 22 (2): 1247-50. [PMID:22172702]

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. Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD et al.. (2012) Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J. Med. Chem., 55 (10): 4580-93. [PMID:22564207]

6. Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN et al.. (2014) Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. J. Med. Chem., 57 (4): 1170-87. [PMID:24432909]

7. 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

Fer family: FER tyrosine kinase. Last modified on 16/02/2017. Accessed on 21/03/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2022.