Details of the Target

General Information of Target

Target ID LDTP12483
Target Name Rho guanine nucleotide exchange factor 3 (ARHGEF3)
Gene Name ARHGEF3
Gene ID 50650
Synonyms
Rho guanine nucleotide exchange factor 3; Exchange factor found in platelets and leukemic and neuronal tissues; XPLN
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MPWEEPAGEKPSCSHSQKAFHMEPAQKPCFTTDMVTWALLCISAETVRGEAPSQPRGIPH
RSPVSVDDLWLEKTQRKKLQKQAHVERRLHIGAVHKDGVKCWRKTIITSPESLNLPRRSH
PLSQSAPTGLNHMGWPEHTPGTAMPDGALDTAVCADEVGSEEDLYDDLHSSSHHYSHPGG
GGEQLAINELISDGSVVCAEALWDHVTMDDQELGFKAGDVIEVMDATNREWWWGRVADGE
GWFPASFVRLRVNQDEPADDDAPLAGNSGAEDGGAEAQSSKDQMRTNVINEILSTERDYI
KHLRDICEGYVRQCRKRADMFSEEQLRTIFGNIEDIYRCQKAFVKALEQRFNRERPHLSE
LGACFLEHQADFQIYSEYCNNHPNACVELSRLTKLSKYVYFFEACRLLQKMIDISLDGFL
LTPVQKICKYPLQLAELLKYTHPQHRDFKDVEAALHAMKNVAQLINERKRRLENIDKIAQ
WQSSIEDWEGEDLLVRSSELIYSGELTRVTQPQAKSQQRMFFLFDHQLIYCKKDLLRRDV
LYYKGRLDMDGLEVVDLEDGKDRDLHVSIKNAFRLHRGATGDSHLLCTRKPEQKQRWLKA
FAREREQVQLDQETGFSITELQRKQAMLNASKQQVTGKPKAVGRPCYLTRQKHPALPSNR
PQQQVLVLAEPRRKPSTFWHSISRLAPFRK
Target Type
Literature-reported
Target Bioclass
Other
Subcellular location
Cytoplasm
Function Acts as a guanine nucleotide exchange factor (GEF) for RhoA and RhoB GTPases.
TTD ID
T96393
Uniprot ID
Q9NR81
DrugMap ID
TT1R5DZ
Ensemble ID
ENST00000296315.8
HGNC ID
HGNC:683

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.R271Ter .
A549 SNV: p.R409I .
JHH4 Insertion: p.A147GfsTer4 .
JURKAT SNV: p.R401Ter .
LOXIMVI SNV: p.A455V .
MELJUSO Substitution: p.P23S .
NB1 SNV: p.P199T .
NCIH661 SNV: p.G456V .
RH30 SNV: p.A28S .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
DBIA
 Probe Info  		C548(1.39)  LDD3313  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [3]
TFBX
 Probe Info  		N.A.  LDD0148  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A101D C548(1.44)  LDD2250  [2]
 LDCM0023  KB03 A375.S2 C548(1.83)  LDD2673  [2]
 LDCM0024  KB05 Hs 936.T C548(1.39)  LDD3313  [2]

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
E3 ubiquitin-protein ligase TRIM23 (TRIM23) Arf family P36406
Zinc finger protein RFP (TRIM27) TRIM/RBCC family P14373
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Pre-B-cell leukemia transcription factor 4 (PBX4) TALE/PBX homeobox family Q9BYU1
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA damage-inducible transcript 4-like protein (DDIT4L) DDIT4 family Q96D03
Centrosomal protein of 70 kDa (CEP70) . Q8NHQ1
Heat shock factor 2-binding protein (HSF2BP) . O75031
PRKCA-binding protein (PICK1) . Q9NRD5

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 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
3 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
4 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