Details of the Target

General Information of Target

Target ID LDTP04510
Target Name Rho GDP-dissociation inhibitor 1 (ARHGDIA)
Gene Name ARHGDIA
Gene ID 396
Synonyms
GDIA1; Rho GDP-dissociation inhibitor 1; Rho GDI 1; Rho-GDI alpha
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAEQEPTAEQLAQIAAENEEDEHSVNYKPPAQKSIQEIQELDKDDESLRKYKEALLGRVA
VSADPNVPNVVVTGLTLVCSSAPGPLELDLTGDLESFKKQSFVLKEGVEYRIKISFRVNR
EIVSGMKYIQHTYRKGVKIDKTDYMVGSYGPRAEEYEFLTPVEEAPKGMLARGSYSIKSR
FTDDDKTDHLSWEWNLTIKKDWKD
Target Bioclass
Other
Family
Rho GDI family
Subcellular location
Cytoplasm
Function
Controls Rho proteins homeostasis. Regulates the GDP/GTP exchange reaction of the Rho proteins by inhibiting the dissociation of GDP from them, and the subsequent binding of GTP to them. Retains Rho proteins such as CDC42, RAC1 and RHOA in an inactive cytosolic pool, regulating their stability and protecting them from degradation. Actively involved in the recycling and distribution of activated Rho GTPases in the cell, mediates extraction from membranes of both inactive and activated molecules due its exceptionally high affinity for prenylated forms. Through the modulation of Rho proteins, may play a role in cell motility regulation. In glioma cells, inhibits cell migration and invasion by mediating the signals of SEMA5A and PLXNB3 that lead to inactivation of RAC1.
Uniprot ID
P52565
Ensemble ID
ENST00000269321.12
HGNC ID
HGNC:678
ChEMBL ID
CHEMBL3638327

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.R120Ter .
HEC1B SNV: p.R120Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 36 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
P8
 Probe Info  		1.79  LDD0451  [1]
A-EBA
 Probe Info  		4.17  LDD0215  [2]
CY4
 Probe Info  		100.00  LDD0244  [3]
C-Sul
 Probe Info  		2.63  LDD0066  [4]
TH211
 Probe Info  		Y133(16.10)  LDD0257  [5]
TH214
 Probe Info  		Y128(15.49); Y51(12.49)  LDD0258  [5]
YN-1
 Probe Info  		100.00  LDD0444  [6]
AZ-9
 Probe Info  		E164(1.37); E154(1.35)  LDD2208  [7]
ONAyne
 Probe Info  		K52(0.00); K178(0.00)  LDD0273  [8]
OPA-S-S-alkyne
 Probe Info  		K43(1.51); K52(1.66); K178(3.53)  LDD3494  [9]
Probe 1
 Probe Info  		Y110(29.04); Y133(24.90); Y149(41.01); Y156(56.28)  LDD3495  [10]
AF-1
 Probe Info  		1.91  LDD0421  [11]
m-APA
 Probe Info  		10.37  LDD0403  [12]
DBIA
 Probe Info  		C79(1.01)  LDD3361  [13]
JZ128-DTB
 Probe Info  		N.A.  LDD0462  [14]
THZ1-DTB
 Probe Info  		C79(1.15)  LDD0460  [14]
DA-P3
 Probe Info  		11.08  LDD0183  [15]
HHS-482
 Probe Info  		Y128(1.00); Y133(1.01); Y144(1.27); Y149(0.73)  LDD0285  [16]
HHS-475
 Probe Info  		Y144(0.80); Y133(0.92); Y51(1.32)  LDD0264  [17]
HHS-465
 Probe Info  		Y133(9.35); Y144(3.57); Y156(5.71)  LDD2237  [18]
Acrolein
 Probe Info  		N.A.  LDD0221  [19]
ATP probe
 Probe Info  		K178(0.00); K141(0.00); K138(0.00); K167(0.00)  LDD0199  [20]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [21]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [21]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [22]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [21]
ATP probe
 Probe Info  		K141(0.00); K167(0.00); K52(0.00); K127(0.00)  LDD0035  [23]
NAIA_4
 Probe Info  		N.A.  LDD2226  [24]
NHS
 Probe Info  		N.A.  LDD0010  [25]
SF
 Probe Info  		Y133(0.00); K178(0.00); K135(0.00)  LDD0028  [26]
STPyne
 Probe Info  		N.A.  LDD0009  [25]
Ox-W18
 Probe Info  		N.A.  LDD2175  [27]
1c-yne
 Probe Info  		K43(0.00); K28(0.00)  LDD0228  [28]
Methacrolein
 Probe Info  		N.A.  LDD0218  [19]
AOyne
 Probe Info  		9.50  LDD0443  [29]
NAIA_5
 Probe Info  		N.A.  LDD2223  [24]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C282
 Probe Info  		17.03  LDD1952  [30]
Photocelecoxib
 Probe Info  		V162(0.00); E163(0.00)  LDD0019  [31]
DA-2
 Probe Info  		N.A.  LDD0070  [32]
STS-1
 Probe Info  		N.A.  LDD0068  [33]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C79(0.91)  LDD1507  [34]
 LDCM0276  AC17 HEK-293T C79(1.15)  LDD1515  [34]
 LDCM0285  AC25 HEK-293T C79(1.08)  LDD1524  [34]
 LDCM0294  AC33 HEK-293T C79(1.02)  LDD1533  [34]
 LDCM0303  AC41 HEK-293T C79(0.85)  LDD1542  [34]
 LDCM0311  AC49 HEK-293T C79(1.02)  LDD1550  [34]
 LDCM0320  AC57 HEK-293T C79(0.75)  LDD1559  [34]
 LDCM0166  Afatinib A431 1.91  LDD0421  [11]
 LDCM0356  AKOS034007680 HEK-293T C79(1.06)  LDD1570  [34]
 LDCM0156  Aniline NCI-H1299 10.37  LDD0403  [12]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [19]
 LDCM0404  CL17 HEK-293T C79(1.14)  LDD1608  [34]
 LDCM0417  CL29 HEK-293T C79(1.31)  LDD1621  [34]
 LDCM0431  CL41 HEK-293T C79(1.17)  LDD1635  [34]
 LDCM0440  CL5 HEK-293T C79(1.01)  LDD1644  [34]
 LDCM0444  CL53 HEK-293T C79(1.00)  LDD1647  [34]
 LDCM0457  CL65 HEK-293T C79(1.04)  LDD1660  [34]
 LDCM0470  CL77 HEK-293T C79(1.03)  LDD1673  [34]
 LDCM0483  CL89 HEK-293T C79(0.86)  LDD1686  [34]
 LDCM0031  Epigallocatechin gallate HEK-293T 11.08  LDD0183  [15]
 LDCM0116  HHS-0101 DM93 Y144(0.80); Y133(0.92); Y51(1.32)  LDD0264  [17]
 LDCM0117  HHS-0201 DM93 Y144(0.67); Y133(0.89); Y51(1.11)  LDD0265  [17]
 LDCM0118  HHS-0301 DM93 Y133(0.87); Y51(0.99); Y144(1.38)  LDD0266  [17]
 LDCM0119  HHS-0401 DM93 Y51(0.73); Y133(0.98); Y144(1.50)  LDD0267  [17]
 LDCM0120  HHS-0701 DM93 Y144(0.82); Y133(0.89); Y51(1.04)  LDD0268  [17]
 LDCM0107  IAA HeLa N.A.  LDD0221  [19]
 LDCM0123  JWB131 DM93 Y128(1.00); Y133(1.01); Y144(1.27); Y149(0.73)  LDD0285  [16]
 LDCM0124  JWB142 DM93 Y128(0.50); Y133(1.09); Y144(1.57); Y149(0.97)  LDD0286  [16]
 LDCM0125  JWB146 DM93 Y128(0.89); Y133(0.92); Y144(1.09); Y149(0.59)  LDD0287  [16]
 LDCM0126  JWB150 DM93 Y128(5.61); Y133(3.59); Y144(0.12); Y149(1.76)  LDD0288  [16]
 LDCM0127  JWB152 DM93 Y128(2.41); Y133(2.03); Y144(2.10); Y149(1.25)  LDD0289  [16]
 LDCM0128  JWB198 DM93 Y128(0.75); Y133(1.81); Y144(0.60); Y149(0.13)  LDD0290  [16]
 LDCM0129  JWB202 DM93 Y128(0.53); Y133(1.16); Y144(1.20); Y149(0.61)  LDD0291  [16]
 LDCM0130  JWB211 DM93 Y128(0.94); Y133(1.30); Y144(0.67); Y149(0.40)  LDD0292  [16]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [14]
 LDCM0022  KB02 Calu-1 C79(1.12)  LDD2292  [13]
 LDCM0023  KB03 Calu-1 C79(1.04)  LDD2709  [13]
 LDCM0024  KB05 NCI-H358 C79(1.01)  LDD3361  [13]
 LDCM0109  NEM HeLa N.A.  LDD0223  [19]
 LDCM0021  THZ1 HeLa S3 C79(1.15)  LDD0460  [14]

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
Ras-related C3 botulinum toxin substrate 1 (RAC1) Rho family P63000
Transforming protein RhoA (RHOA) Rho family P61586
Cell division control protein 42 homolog (CDC42) Rho family P60953
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tumor necrosis factor receptor superfamily member 19 (TNFRSF19) . Q9NS68
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
TERF1-interacting nuclear factor 2 (TINF2) . Q9BSI4

References

1 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
2 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
3 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.
4 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
5 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
6 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
7 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.
8 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
9 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
10 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
11 Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening. Chem Commun (Camb). 2019 Jan 15;55(6):834-837. doi: 10.1039/c8cc08685k.
12 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.
13 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
14 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
15 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
16 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
17 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.
18 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.
19 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.
20 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
21 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
22 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
23 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
24 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
25 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
26 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
27 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
28 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
29 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
30 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
31 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094
32 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
33 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
34 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402