Details of the Target

General Information of Target

Target ID LDTP08127
Target Name Arpin (ARPIN)
Gene Name ARPIN
Gene ID 348110
Synonyms
C15orf38; Arpin; Arp2/3 inhibition protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSRIYHDGALRNKAVQSVRLPGAWDPAAHQGGNGVLLEGELIDVSRHSILDTHGRKERYY
VLYIRPSHIHRRKFDAKGNEIEPNFSATRKVNTGFLMSSYKVEAKGDTDRLTPEALKGLV
NKPELLALTESLTPDHTVAFWMPESEMEVMELELGAGVRLKTRGDGPFLDSLAKLEAGTV
TKCNFTGDGKTGASWTDNIMAQKCSKGAAAEIREQGDGAEDEEWDD
Target Bioclass
Other
Family
Arpin family
Subcellular location
Cell projection, lamellipodium
Function
Regulates actin polymerization by inhibiting the actin-nucleating activity of the Arp2/3 complex; the function is competitive with nucleation promoting factors. Participates in an incoherent feedforward loop at the lamellipodium tip where it inhibits the ARP2/2 complex in response to Rac signaling and where Rac also stimulates actin polymerization through the WAVE complex. Involved in steering cell migration by controlling its directional persistence.
Uniprot ID
Q7Z6K5
Ensemble ID
ENST00000357484.10
HGNC ID
HGNC:28782

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
MEC1 SNV: p.K13N .
OVISE SNV: p.L50S .
REH SNV: p.R11P .
SNU1 SNV: p.S48N .
TOV21G SNV: p.Ter227LextTer53 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C183(2.94)  LDD3493  [1]
HHS-475
 Probe Info  		Y5(1.13)  LDD0264  [2]
HHS-465
 Probe Info  		Y5(10.00)  LDD2237  [3]
m-APA
 Probe Info  		N.A.  LDD2231  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [5]
NAIA_4
 Probe Info  		N.A.  LDD2226  [6]
TFBX
 Probe Info  		N.A.  LDD0027  [7]
WYneN
 Probe Info  		N.A.  LDD0021  [8]
IPM
 Probe Info  		N.A.  LDD0005  [8]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C183(1.13)  LDD1702  [10]
 LDCM0116  HHS-0101 DM93 Y5(1.13)  LDD0264  [2]
 LDCM0117  HHS-0201 DM93 Y5(0.63)  LDD0265  [2]
 LDCM0118  HHS-0301 DM93 Y5(0.37)  LDD0266  [2]
 LDCM0120  HHS-0701 DM93 Y5(0.17)  LDD0268  [2]
 LDCM0022  KB02 AU565 C183(4.43)  LDD2265  [1]
 LDCM0023  KB03 MDA-MB-231 C183(2.34)  LDD1701  [10]
 LDCM0024  KB05 ZR-75-1 C183(2.94)  LDD3493  [1]
 LDCM0627  NUDT7-COV-1 HEK-293T C183(0.66)  LDD2206  [11]
 LDCM0628  OTUB2-COV-1 HEK-293T C183(0.63); C183(0.18)  LDD2207  [11]

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
Poly [ADP-ribose] polymerase tankyrase-2 (TNKS2) ARTD/PARP family Q9H2K2
NIF3-like protein 1 (NIF3L1) GTP cyclohydrolase I type 2/NIF3 family Q9GZT8
Zinc finger protein RFP (TRIM27) TRIM/RBCC family P14373
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Actin-related protein 2/3 complex subunit 2 (ARPC2) ARPC2 family O15144
DNA damage-inducible transcript 4-like protein (DDIT4L) DDIT4 family Q96D03

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 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
3 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
4 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
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 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
7 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
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 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
10 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
11 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.