Details of the Target

General Information of Target

Target ID LDTP06342
Target Name Receptor-type tyrosine-protein phosphatase R (PTPRR)
Gene Name PTPRR
Gene ID 5801
Synonyms
ECPTP; PTPRQ; Receptor-type tyrosine-protein phosphatase R; R-PTP-R; EC 3.1.3.48; Ch-1PTPase; NC-PTPCOM1; Protein-tyrosine phosphatase PCPTP1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRRAVCFPALCLLLNLHAAGCFSGNNDHFLAINQKKSGKPVFIYKHSQDIEKSLDIAPQK
IYRHSYHSSSEAQVSKRHQIVNSAFPRPAYDPSLNLLAMDGQDLEVENLPIPAANVIVVT
LQMDVNKLNITLLRIFRQGVAAALGLLPQQVHINRLIGKKNSIELFVSPINRKTGISDAL
PSEEVLRSLNINVLHQSLSQFGITEVSPEKNVLQGQHEADKIWSKEGFYAVVIFLSIFVI
IVTCLMILYRLKERFQLSLRQDKEKNQEIHLSPITLQPALSEAKTVHSMVQPEQAPKVLN
VVVDPQGRGAPEIKATTATSVCPSPFKMKPIGLQERRGSNVSLTLDMSSLGNIEPFVSIP
TPREKVAMEYLQSASRILTRSQLRDVVASSHLLQSEFMEIPMNFVDPKEIDIPRHGTKNR
YKTILPNPLSRVCLRPKNVTDSLSTYINANYIRGYSGKEKAFIATQGPMINTVDDFWQMV
WQEDSPVIVMITKLKEKNEKCVLYWPEKRGIYGKVEVLVISVNECDNYTIRNLVLKQGSH
TQHVKHYWYTSWPDHKTPDSAQPLLQLMLDVEEDRLASQGRGPVVVHCSAGIGRTGCFIA
TSIGCQQLKEEGVVDALSIVCQLRMDRGGMVQTSEQYEFVHHALCLYESRLSAETVQ
Target Bioclass
Enzyme
Family
Protein-tyrosine phosphatase family, Receptor class 7 subfamily
Subcellular location
Secreted; Cytoplasm, perinuclear region; Cell membrane
Function
Sequesters mitogen-activated protein kinases (MAPKs) such as MAPK1, MAPK3 and MAPK14 in the cytoplasm in an inactive form. The MAPKs bind to a dephosphorylated kinase interacting motif, phosphorylation of which by the protein kinase A complex releases the MAPKs for activation and translocation into the nucleus.
Uniprot ID
Q15256
Ensemble ID
ENST00000283228.7
HGNC ID
HGNC:9680
ChEMBL ID
CHEMBL3425390

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CALU1 SNV: p.D526N .
CCK81 SNV: p.L271P .
G402 SNV: p.N450S .
HCT15 SNV: p.N266K .
HEC1 SNV: p.D559N .
HEC1B SNV: p.D559N .
HT115 SNV: p.R187C .
IGR1 SNV: p.E107K .
JURKAT SNV: p.M402T .
LS180 Deletion: p.N438MfsTer2 .
NCIH1793 SNV: p.G38V .
OVK18 SNV: p.L443F .
SKMEL2 SNV: p.S342F .
SNGM Deletion: p.N498MfsTer25 .
SNU1 SNV: p.Q622R .
TE4 SNV: p.S75T .
TF1 SNV: p.I135M .
UACC62 SNV: p.M123I .

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  		C605(2.99)  LDD3338  [1]
NAIA_5
 Probe Info  		N.A.  LDD2225  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 HG-3 C605(3.02)  LDD2355  [1]
 LDCM0023  KB03 HG-3 C605(5.31)  LDD2772  [1]
 LDCM0024  KB05 MV4-11 C605(2.99)  LDD3338  [1]

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 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264