Details of the Target

General Information of Target

Target ID LDTP08091
Target Name Rho GTPase-activating protein 22 (ARHGAP22)
Gene Name ARHGAP22
Gene ID 58504
Synonyms
RHOGAP2; Rho GTPase-activating protein 22; Rho-type GTPase-activating protein 22
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLSPKIRQARRARSKSLVMGEQSRSPGRMPCPHRLGPVLKAGWLKKQRSIMKNWQQRWFV
LRGDQLFYYKDKDEIKPQGFISLQGTQVTELPPGPEDPGKHLFEISPGGAGEREKVPANP
EALLLMASSQRDMEDWVQAIRRVIWAPLGGGIFGQRLEETVHHERKYGPRLAPLLVEQCV
DFIRERGLTEEGLFRMPGQANLVRDLQDSFDCGEKPLFDSTTDVHTVASLLKLYLRELPE
PVVPFARYEDFLSCAQLLTKDEGEGTLELAKQVSNLPQANYNLLRYICKFLDEVQAYSNV
NKMSVQNLATVFGPNILRPQVEDPVTIMEGTSLVQHLMTVLIRKHSQLFTAPVPEGPTSP
RGGLQCAVGWGSEEVTRDSQGEPGGPGLPAHRTSSLDGAAVAVLSRTAPTGPGSRCSPGK
KVQTLPSWKSSFRQPRSLSGSPKGGGSSLEVPIISSGGNWLMNGLSSLRGHRRASSGDRL
KDSGSVQRLSTYDNVPAPGLVPGIPSVASMAWSGASSSESSVGGSLSSCTACRASDSSAR
SSLHTDWALEPSPLPSSSEDPKSLDLDHSMDEAGAGASNSEPSEPDSPTREHARRSEALQ
GLVTELRAELCRQRTEYERSVKRIEEGSADLRKRMSRLEEELDQEKKKYIMLEIKLRNSE
RAREDAERRNQLLQREMEEFFSTLGSLTVGAKGARAPK
Target Bioclass
Other
Subcellular location
Cytoplasm
Function
Rho GTPase-activating protein involved in the signal transduction pathway that regulates endothelial cell capillary tube formation during angiogenesis. Acts as a GTPase activator for the RAC1 by converting it to an inactive GDP-bound state. Inhibits RAC1-dependent lamellipodia formation. May also play a role in transcription regulation via its interaction with VEZF1, by regulating activity of the endothelin-1 (EDN1) promoter.
Uniprot ID
Q7Z5H3
Ensemble ID
ENST00000249601.9
HGNC ID
HGNC:30320

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 SNV: p.G693D .
COLO800 SNV: p.H162Y .
CORL23 SNV: p.D97N .
HCT15 SNV: p.P418H .
J82 SNV: p.E112D .
LS180 Deletion: p.S682RfsTer3
SNV: p.S274N		 .
LU65 SNV: p.E519V .
MDAMB468 SNV: p.I327L .
NCIH1793 SNV: p.R156L .
NCIH661 SNV: p.W547L .
ONS76 SNV: p.K5N .
RKO Insertion: p.G446RfsTer160
SNV: p.R34K		 .
RPMI8226 SNV: p.K70N .
SW1271 SNV: p.W145C .
SW480 SNV: p.G63E .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K5(0.55)  LDD0277  [1]
DBIA
 Probe Info  		C89(1.66)  LDD3335  [2]
IPM
 Probe Info  		N.A.  LDD2156  [3]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [4]
AOyne
 Probe Info  		15.00  LDD0443  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C366(1.21)  LDD1507  [6]
 LDCM0226  AC11 HEK-293T C366(1.56)  LDD1509  [6]
 LDCM0276  AC17 HEK-293T C366(1.03)  LDD1515  [6]
 LDCM0278  AC19 HEK-293T C366(1.44)  LDD1517  [6]
 LDCM0281  AC21 HEK-293T C366(1.34)  LDD1520  [6]
 LDCM0285  AC25 HEK-293T C366(0.95)  LDD1524  [6]
 LDCM0287  AC27 HEK-293T C366(1.46)  LDD1526  [6]
 LDCM0289  AC29 HEK-293T C366(1.10)  LDD1528  [6]
 LDCM0290  AC3 HEK-293T C366(1.61)  LDD1529  [6]
 LDCM0294  AC33 HEK-293T C366(1.14)  LDD1533  [6]
 LDCM0296  AC35 HEK-293T C366(1.49)  LDD1535  [6]
 LDCM0298  AC37 HEK-293T C366(0.96)  LDD1537  [6]
 LDCM0303  AC41 HEK-293T C366(0.89)  LDD1542  [6]
 LDCM0305  AC43 HEK-293T C366(1.71)  LDD1544  [6]
 LDCM0307  AC45 HEK-293T C366(0.89)  LDD1546  [6]
 LDCM0311  AC49 HEK-293T C366(0.96)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C366(0.97)  LDD1551  [6]
 LDCM0314  AC51 HEK-293T C366(1.66)  LDD1553  [6]
 LDCM0316  AC53 HEK-293T C366(1.01)  LDD1555  [6]
 LDCM0320  AC57 HEK-293T C366(0.99)  LDD1559  [6]
 LDCM0322  AC59 HEK-293T C366(1.52)  LDD1561  [6]
 LDCM0325  AC61 HEK-293T C366(0.90)  LDD1564  [6]
 LDCM0248  AKOS034007472 HEK-293T C366(0.95)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C366(1.05)  LDD1570  [6]
 LDCM0404  CL17 HEK-293T C366(1.10)  LDD1608  [6]
 LDCM0406  CL19 HEK-293T C366(1.43)  LDD1610  [6]
 LDCM0409  CL21 HEK-293T C366(1.41)  LDD1613  [6]
 LDCM0417  CL29 HEK-293T C366(0.98)  LDD1621  [6]
 LDCM0420  CL31 HEK-293T C366(1.48)  LDD1624  [6]
 LDCM0422  CL33 HEK-293T C366(1.19)  LDD1626  [6]
 LDCM0431  CL41 HEK-293T C366(1.02)  LDD1635  [6]
 LDCM0433  CL43 HEK-293T C366(1.36)  LDD1637  [6]
 LDCM0435  CL45 HEK-293T C366(1.14)  LDD1639  [6]
 LDCM0440  CL5 HEK-293T C366(1.11)  LDD1644  [6]
 LDCM0444  CL53 HEK-293T C366(1.32)  LDD1647  [6]
 LDCM0446  CL55 HEK-293T C366(1.49)  LDD1649  [6]
 LDCM0448  CL57 HEK-293T C366(1.46)  LDD1651  [6]
 LDCM0457  CL65 HEK-293T C366(1.16)  LDD1660  [6]
 LDCM0459  CL67 HEK-293T C366(1.47)  LDD1662  [6]
 LDCM0461  CL69 HEK-293T C366(1.09)  LDD1664  [6]
 LDCM0462  CL7 HEK-293T C366(1.60)  LDD1665  [6]
 LDCM0470  CL77 HEK-293T C366(0.95)  LDD1673  [6]
 LDCM0472  CL79 HEK-293T C366(1.51)  LDD1675  [6]
 LDCM0475  CL81 HEK-293T C366(1.27)  LDD1678  [6]
 LDCM0483  CL89 HEK-293T C366(1.01)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C366(1.21)  LDD1687  [6]
 LDCM0486  CL91 HEK-293T C366(1.47)  LDD1689  [6]
 LDCM0488  CL93 HEK-293T C366(1.05)  LDD1691  [6]
 LDCM0022  KB02 CMK C89(1.36)  LDD2302  [2]
 LDCM0023  KB03 CMK C89(2.41)  LDD2719  [2]
 LDCM0024  KB05 MONO-MAC-6 C89(1.66)  LDD3335  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Voltage-dependent P/Q-type calcium channel subunit alpha-1A (CACNA1A) Calcium channel alpha-1 subunit (TC 1.A.1.11) family O00555
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-D1-binding protein 1 (CCNDBP1) CCNDBP1 family O95273
Differentially expressed in FDCP 6 homolog (DEF6) . Q9H4E7

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 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 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
4 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
5 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.
6 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