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FER tyrosine kinase

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Target id: 2022

Nomenclature: FER tyrosine kinase

Abbreviated Name: Fer

Family: Fer family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 822 5q21.3 FER FER tyrosine kinase
Mouse - 823 17 E1.1 Fer FER tyrosine kinase
Rat - 823 9q37 Fer FER tyrosine kinase
Previous and Unofficial Names Click here for help
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 | fer (fms/fps related) protein kinase
Database Links Click here for help
Alphafold P16591 (Hs), P70451 (Mm), P09760 (Rn)
BRENDA 2.7.10.2
CATH/Gene3D 3.30.505.10
ChEMBL Target CHEMBL3982 (Hs), CHEMBL4523172 (Rn)
Ensembl Gene ENSG00000151422 (Hs), ENSMUSG00000000127 (Mm), ENSRNOG00000015898 (Rn)
Entrez Gene 2241 (Hs), 14158 (Mm), 301737 (Rn)
Human Protein Atlas ENSG00000151422 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:2241 (Hs), mmu:14158 (Mm), rno:301737 (Rn)
OMIM 176942 (Hs)
Pharos P16591 (Hs)
RefSeq Nucleotide NM_005246 (Hs), NM_001037997 (Mm), NM_001106928 (Rn)
RefSeq Protein NP_005237 (Hs), NP_001033086 (Mm), NP_001100398 (Rn)
UniProtKB P16591 (Hs), P70451 (Mm), P09760 (Rn)
Wikipedia FER (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.10.2

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
Ro3280 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pKd 2
⤷ pKd 7.3 (Kd 5.3x10-8 M) [2]
Description: Ambit selectivity screen at 1μM Ro3280.
DS21360717 Small molecule or natural product Hs Inhibition 9.3 pIC50 7
⤷ pIC50 9.3 (IC50 4.9x10-10 M) [7]
Description: Measuring inhibition of FL-Peptide22 substrate phosphorylation by recombinant N-terminal-His-tagged fragment of FER (from SH2 domain to C-terminal) using a Labchip EZ Reader II.
compound 8e [PMID: 24432909] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 6
⤷ pIC50 8.7 (IC50 2x10-9 M) [6]
compound 25b [PMID: 22564207] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 5
⤷ pIC50 7.1 (IC50 8.5x10-8 M) [5]
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: 3,8
Key to terms and symbols Click column headers to sort
Target used in screen: FER
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
GSK-1838705A Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand 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 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: 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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.8 2.0 0.5
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.8 2.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 5.4 33.0 20.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 4.0 4.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 17.7 79.0 14.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 20.0 35.0 9.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 21.7 23.0 1.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 22.4 26.0 14.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 28.8 37.0 35.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure 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
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling

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. Taniguchi T, Inagaki H, Baba D, Yasumatsu I, Toyota A, Kaneta Y, Kiga M, Iimura S, Odagiri T, Shibata Y et al.. (2019) Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity. ACS Med Chem Lett, 10 (5): 737-742. DOI: 10.1021/acsmedchemlett.8b00631 [PMID:31097992]

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

Fer family: FER tyrosine kinase. Last modified on 23/04/2019. Accessed on 11/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2022.