Details of the Target

General Information of Target

Target ID LDTP03361
Target Name Protein S100-A4 (S100A4)
Gene Name S100A4
Gene ID 6275
Synonyms
CAPL; MTS1; Protein S100-A4; Calvasculin; Metastasin; Placental calcium-binding protein; Protein Mts1; S100 calcium-binding protein A4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MACPLEKALDVMVSTFHKYSGKEGDKFKLNKSELKELLTRELPSFLGKRTDEAAFQKLMS
NLDSNRDNEVDFQEYCVFLSCIAMMCNEFFEGFPDKQPRKK
Target Type
Literature-reported
Target Bioclass
Other
Family
S-100 family
Subcellular location
Secreted
Function
Calcium-binding protein that plays a role in various cellular processes including motility, angiogenesis, cell differentiation, apoptosis, and autophagy. Increases cell motility and invasiveness by interacting with non-muscle myosin heavy chain (NMMHC) IIA/MYH9. Mechanistically, promotes filament depolymerization and increases the amount of soluble myosin-IIA, resulting in the formation of stable protrusions facilitating chemotaxis. Modulates also the pro-apoptotic function of TP53 by binding to its C-terminal transactivation domain within the nucleus and reducing its protein levels. Within the extracellular space, stimulates cytokine production including granulocyte colony-stimulating factor and CCL24 from T-lymphocytes. In addition, stimulates T-lymphocyte chemotaxis by acting as a chemoattractant complex with PGLYRP1 that promotes lymphocyte migration via CCR5 and CXCR3 receptors.
TTD ID
T35265
Uniprot ID
P26447
DrugMap ID
TTPR5SX
Ensemble ID
ENST00000354332.8
HGNC ID
HGNC:10494
ChEMBL ID
CHEMBL2362976

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 16 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
ONAyne
 Probe Info  		K22(2.30); K31(0.31); K35(0.44); K48(1.01)  LDD0274  [1]
STPyne
 Probe Info  		K18(9.70); K22(5.33); K26(6.29); K28(3.41)  LDD0277  [1]
OPA-S-S-alkyne
 Probe Info  		K57(3.85); K48(5.05); K35(6.43)  LDD3494  [2]
5E-2FA
 Probe Info  		N.A.  LDD2235  [3]
m-APA
 Probe Info  		N.A.  LDD2231  [3]
CY-1
 Probe Info  		N.A.  LDD0246  [4]
AZ-9
 Probe Info  		N.A.  LDD0395  [5]
IPM
 Probe Info  		N.A.  LDD0025  [6]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [6]
NAIA_4
 Probe Info  		N.A.  LDD2226  [7]
NAIA_5
 Probe Info  		N.A.  LDD2224  [7]
WYneN
 Probe Info  		N.A.  LDD0021  [8]
IA-alkyne
 Probe Info  		C86(0.00); C81(0.00); C76(0.00)  LDD0151  [9]
TFBX
 Probe Info  		N.A.  LDD0148  [6]
Acrolein
 Probe Info  		N.A.  LDD0217  [10]
HHS-465
 Probe Info  		K22(0.00); K35(0.00); K31(0.00); K48(0.00)  LDD2240  [11]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
KIRA6 AfBP
 Probe Info  		N.A.  LDD0378  [12]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [10]
 LDCM0107  IAA HeLa N.A.  LDD0221  [10]
 LDCM0024  KB05 T cell C76, C81, C86(6.02)  LDD1709  [13]
 LDCM0109  NEM HeLa N.A.  LDD0223  [10]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 ubiquitin-protein ligase Mdm2 (MDM2) MDM2/MDM4 family Q00987
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Receptor tyrosine-protein kinase erbB-3 (ERBB3) Tyr protein kinase family P21860
Receptor tyrosine-protein kinase erbB-4 (ERBB4) Tyr protein kinase family Q15303
Myosin-9 (MYH9) Myosin family P35579
Calcyclin-binding protein (CACYBP) . Q9HB71
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Protein S100-A1 (S100A1) S-100 family P23297
Protein S100-B (S100B) S-100 family P04271
Transient receptor potential cation channel subfamily M member 4 (TRPM4) Transient receptor (TC 1.A.4) family Q8TD43
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amphiregulin (AREG) Amphiregulin family P15514
Protein S100-A4 (S100A4) S-100 family P26447
Ezrin (EZR) . P15311
Probetacellulin (BTC) . P35070

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Trifluoperazine Small molecular drug DB00831
Copper . DB09130
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sp-met-1 . D0U7ZY

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
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 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
5 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
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 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
8 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
9 Sequence-Based Prediction of Cysteine Reactivity Using Machine Learning. Biochemistry. 2018 Jan 30;57(4):451-460. doi: 10.1021/acs.biochem.7b00897. Epub 2017 Oct 26.
10 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.
11 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
12 Kinase Photoaffinity Labeling Reveals Low Selectivity Profile of the IRE1 Targeting Imidazopyrazine-Based KIRA6 Inhibitor. ACS Chem Biol. 2020 Dec 18;15(12):3106-3111. doi: 10.1021/acschembio.0c00802. Epub 2020 Dec 8.
Mass spectrometry data entry: PXD022628
13 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.