Details of the Target

General Information of Target

Target ID LDTP05404
Target Name Urokinase plasminogen activator surface receptor (PLAUR)
Gene Name PLAUR
Gene ID 5329
Synonyms
MO3; UPAR; Urokinase plasminogen activator surface receptor; U-PAR; uPAR; Monocyte activation antigen Mo3; CD antigen CD87
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGHPPLLPLLLLLHTCVPASWGLRCMQCKTNGDCRVEECALGQDLCRTTIVRLWEEGEEL
ELVEKSCTHSEKTNRTLSYRTGLKITSLTEVVCGLDLCNQGNSGRAVTYSRSRYLECISC
GSSDMSCERGRHQSLQCRSPEEQCLDVVTHWIQEGEEGRPKDDRHLRGCGYLPGCPGSNG
FHNNDTFHFLKCCNTTKCNEGPILELENLPQNGRQCYSCKGNSTHGCSSEETFLIDCRGP
MNQCLVATGTHEPKNQSYMVRGCATASMCQHAHLGDAFSMNHIDVSCCTKSGCNHPDLDV
QYRSGAAPQPGPAHLSLTITLLMTARLWGGTLLWT
Target Type
Successful
Target Bioclass
Other
Subcellular location
Secreted; Cell membrane
Function
Acts as a receptor for urokinase plasminogen activator. Plays a role in localizing and promoting plasmin formation. Mediates the proteolysis-independent signal transduction activation effects of U-PA. It is subject to negative-feedback regulation by U-PA which cleaves it into an inactive form.
TTD ID
T74363
Uniprot ID
Q03405
DrugMap ID
TTPRL03
Ensemble ID
ENST00000221264.8
HGNC ID
HGNC:9053
ChEMBL ID
CHEMBL4883

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.W328Ter .
SUPT1 SNV: p.G32V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
OPA-S-S-alkyne
 Probe Info  		K29(3.61)  LDD3494  [2]
BTD
 Probe Info  		C67(2.77); C137(1.15)  LDD1700  [3]
DBIA
 Probe Info  		C117(1.42); C120(1.42); C127(1.42)  LDD0078  [4]
IA-alkyne
 Probe Info  		C137(0.00); C34(0.00); C144(0.00); C67(0.00)  LDD0162  [5]
TFBX
 Probe Info  		C198(0.00); C34(0.00); C137(0.00)  LDD0148  [6]
Acrolein
 Probe Info  		N.A.  LDD0217  [7]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [7]
Methacrolein
 Probe Info  		C39(0.00); C137(0.00); C293(0.00); C46(0.00)  LDD0218  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C67(0.60)  LDD2095  [3]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C67(0.82)  LDD2130  [3]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C67(0.81); C137(0.65)  LDD2117  [3]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C244(2.27); C137(1.02)  LDD2152  [3]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C67(0.37)  LDD2131  [3]
 LDCM0545  Acetamide MDA-MB-231 C67(0.41)  LDD2138  [3]
 LDCM0520  AKOS000195272 MDA-MB-231 C67(1.06); C244(1.32); C137(0.68)  LDD2113  [3]
 LDCM0156  Aniline NCI-H1299 12.21  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C117(1.42); C120(1.42); C127(1.42)  LDD0078  [4]
 LDCM0498  BS-3668 MDA-MB-231 C67(0.88); C244(0.76); C137(0.42)  LDD2091  [3]
 LDCM0108  Chloroacetamide HeLa C293(0.00); C137(0.00)  LDD0222  [7]
 LDCM0022  KB02 8305C C137(1.52)  LDD2248  [8]
 LDCM0023  KB03 8305C C137(1.86)  LDD2665  [8]
 LDCM0024  KB05 COLO792 C93(2.08)  LDD3310  [8]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C244(0.92); C137(0.62)  LDD2121  [3]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C67(0.64)  LDD2089  [3]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C244(2.56); C137(0.75)  LDD2093  [3]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C244(1.79); C137(0.74)  LDD2097  [3]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C137(0.85); C293(0.74)  LDD2099  [3]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C67(0.88); C244(1.91); C137(1.03); C293(2.00)  LDD2101  [3]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C67(0.76)  LDD2104  [3]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C67(1.01); C244(1.03); C137(0.69)  LDD2107  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C67(1.77); C137(1.01)  LDD2109  [3]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C67(1.01); C244(1.24); C137(0.79); C293(0.81)  LDD2111  [3]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C67(0.45); C244(0.84); C137(0.75)  LDD2115  [3]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C244(2.01)  LDD2119  [3]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C67(1.12); C137(0.80); C293(0.92)  LDD2123  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C67(1.17); C244(1.21); C137(0.45); C293(0.91)  LDD2125  [3]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C293(1.22)  LDD2127  [3]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C67(1.19); C244(1.26); C137(0.77)  LDD2129  [3]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C137(0.52); C293(0.80)  LDD2133  [3]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C67(0.56); C244(1.02); C137(0.40)  LDD2134  [3]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C67(0.98); C137(0.97)  LDD2135  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C244(1.12); C137(0.96)  LDD2136  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C67(1.23)  LDD2137  [3]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C67(2.77); C137(1.15)  LDD1700  [3]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C67(1.26); C137(0.63)  LDD2140  [3]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C67(1.04)  LDD2141  [3]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C244(0.42)  LDD2143  [3]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C67(0.58)  LDD2145  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C67(1.31); C244(1.38); C137(0.58)  LDD2146  [3]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C244(0.51)  LDD2147  [3]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C67(0.85); C244(0.75); C137(0.73); C293(0.43)  LDD2148  [3]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C67(0.58); C244(0.61)  LDD2150  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Angiogenin (ANG) Pancreatic ribonuclease family P03950
Urokinase-type plasminogen activator (PLAU) Peptidase S1 family P00749
Ataxin-3 (ATXN3) . P54252
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Gelsolin (GSN) Villin/gelsolin family P06396
Sprouty-related, EVH1 domain-containing protein 1 (SPRED1) . Q7Z699

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tenecteplase BiotechDrug DB00031
Urokinase BiotechDrug DB00013
Ruxolitinib Small molecular drug D04LKS
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Wx-uk1 Small molecular drug DB05476
Lanoteplase . DB06245

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
5 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
6 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
7 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
8 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