Details of the Target

General Information of Target

Target ID LDTP03992
Target Name Tyrosine-protein kinase FRK (FRK)
Gene Name FRK
Gene ID 2444
Synonyms
PTK5; RAK; Tyrosine-protein kinase FRK; EC 2.7.10.2; FYN-related kinase; Nuclear tyrosine protein kinase RAK; Protein-tyrosine kinase 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSNICQRLWEYLEPYLPCLSTEADKSTVIENPGALCSPQSQRHGHYFVALFDYQARTAED
LSFRAGDKLQVLDTLHEGWWFARHLEKRRDGSSQQLQGYIPSNYVAEDRSLQAEPWFFGA
IGRSDAEKQLLYSENKTGSFLIRESESQKGEFSLSVLDGAVVKHYRIKRLDEGGFFLTRR
RIFSTLNEFVSHYTKTSDGLCVKLGKPCLKIQVPAPFDLSYKTVDQWEIDRNSIQLLKRL
GSGQFGEVWEGLWNNTTPVAVKTLKPGSMDPNDFLREAQIMKNLRHPKLIQLYAVCTLED
PIYIITELMRHGSLQEYLQNDTGSKIHLTQQVDMAAQVASGMAYLESRNYIHRDLAARNV
LVGEHNIYKVADFGLARVFKVDNEDIYESRHEIKLPVKWTAPEAIRSNKFSIKSDVWSFG
ILLYEIITYGKMPYSGMTGAQVIQMLAQNYRLPQPSNCPQQFYNIMLECWNAEPKERPTF
ETLRWKLEDYFETDSSYSDANNFIR
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, SRC subfamily
Subcellular location
Cytoplasm
Function
Non-receptor tyrosine-protein kinase that negatively regulates cell proliferation. Positively regulates PTEN protein stability through phosphorylation of PTEN on 'Tyr-336', which in turn prevents its ubiquitination and degradation, possibly by reducing its binding to NEDD4. May function as a tumor suppressor.
Uniprot ID
P42685
Ensemble ID
ENST00000606080.2
HGNC ID
HGNC:3955
ChEMBL ID
CHEMBL4223

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CASKI SNV: p.R64Q .
GB1 SNV: p.D270V .
HT115 SNV: p.S147R .
MEWO SNV: p.W249R .
SKN Deletion: p.F51IfsTer10 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C59(5.13)  LDD3314  [1]
IA-alkyne
 Probe Info  		C201(0.00); C208(0.00)  LDD0162  [2]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DFG-out-3
 Probe Info  		100.00  LDD0074  [3]
DFG-out-4
 Probe Info  		0.00  LDD0075  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0017  DFG-out-2 A431 0.00  LDD0075  [3]
 LDCM0022  KB02 A498 C36(1.40)  LDD2259  [1]
 LDCM0023  KB03 A498 C36(1.68)  LDD2676  [1]
 LDCM0024  KB05 IGR37 C59(5.13)  LDD3314  [1]
 LDCM0016  Ranjitkar_cp1 A431 100.00  LDD0074  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN (PTEN) PTEN phosphatase protein family P60484
BCL2/adenovirus E1B 19 kDa protein-interacting protein 2 (BNIP2) . Q12982
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
Splicing factor 3B subunit 4 (SF3B4) SF3B4 family Q15427

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dasatinib Small molecular drug DB01254
Fostamatinib Small molecular drug DB12010
Regorafenib Small molecular drug DB08896
Zanubrutinib . DB15035

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
3 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.