General Information of Target

Target ID LDTP08788
Target Name Rho GTPase-activating protein 24 (ARHGAP24)
Gene Name ARHGAP24
Gene ID 83478
Synonyms
FILGAP; Rho GTPase-activating protein 24; Filamin-A-associated RhoGAP; FilGAP; RAC1- and CDC42-specific GTPase-activating protein of 72 kDa; RC-GAP72; Rho-type GTPase-activating protein 24; RhoGAP of 73 kDa; Sarcoma antigen NY-SAR-88; p73RhoGAP
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEENNDSTENPQQGQGRQNAIKCGWLRKQGGFVKTWHTRWFVLKGDQLYYFKDEDETKPL
GTIFLPGNKVSEHPCNEENPGKFLFEVVPGGDRDRMTANHESYLLMASTQNDMEDWVKSI
RRVIWGPFGGGIFGQKLEDTVRYEKRYGNRLAPMLVEQCVDFIRQRGLKEEGLFRLPGQA
NLVKELQDAFDCGEKPSFDSNTDVHTVASLLKLYLRELPEPVIPYAKYEDFLSCAKLLSK
EEEAGVKELAKQVKSLPVVNYNLLKYICRFLDEVQSYSGVNKMSVQNLATVFGPNILRPK
VEDPLTIMEGTVVVQQLMSVMISKHDCLFPKDAELQSKPQDGVSNNNEIQKKATMGQLQN
KENNNTKDSPSRQCSWDKSESPQRSSMNNGSPTALSGSKTNSPKNSVHKLDVSRSPPLMV
KKNPAFNKGSGIVTNGSFSSSNAEGLEKTQTTPNGSLQARRSSSLKVSGTKMGTHSVQNG
TVRMGILNSDTLGNPTNVRNMSWLPNGYVTLRDNKQKEQAGELGQHNRLSTYDNVHQQFS
MMNLDDKQSIDSATWSTSSCEISLPENSNSCRSSTTTCPEQDFFGGNFEDPVLDGPPQDD
LSHPRDYESKSDHRSVGGRSSRATSSSDNSETFVGNSSSNHSALHSLVSSLKQEMTKQKI
EYESRIKSLEQRNLTLETEMMSLHDELDQERKKFTMIEIKMRNAERAKEDAEKRNDMLQK
EMEQFFSTFGELTVEPRRTERGNTIWIQ
Target Bioclass
Other
Subcellular location
Cytoplasm, cytoskeleton
Function
Rho GTPase-activating protein involved in cell polarity, cell morphology and cytoskeletal organization. Acts as a GTPase activator for the Rac-type GTPase by converting it to an inactive GDP-bound state. Controls actin remodeling by inactivating Rac downstream of Rho leading to suppress leading edge protrusion and promotes cell retraction to achieve cellular polarity. Able to suppress RAC1 and CDC42 activity in vitro. Overexpression induces cell rounding with partial or complete disruption of actin stress fibers and formation of membrane ruffles, lamellipodia, and filopodia. Isoform 2 is a vascular cell-specific GAP involved in modulation of angiogenesis.
Uniprot ID
Q8N264
Ensemble ID
ENST00000264343.4
HGNC ID
HGNC:25361

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CASKI SNV: p.F583Y .
CCK81 SNV: p.S371G .
CHL1 SNV: p.D377N .
EOL1 SNV: p.C159S .
FUOV1 SNV: p.W36Ter .
HS936T SNV: p.D533Y .
KYSE150 SNV: p.V160M; p.S638N .
MCC13 SNV: p.E561K .
MCC26 SNV: p.Q187Ter; p.S602F .
MEWO SNV: p.R499Ter DBIA    Probe Info 
MIAPACA2 SNV: p.P11R .
NCIH1155 SNV: p.G30Ter .
NCIH23 SNV: p.L232W .
OPM2 SNV: p.R175Ter .
RKO Insertion: p.M722NfsTer50 .
RL952 SNV: p.R216Ter .
RPMI8226 Substitution: p.E9K .
SBC5 SNV: p.S563F .
SW1990 SNV: p.R216Ter .

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
AHL-Pu-1
 Probe Info 
C578(5.93); C75(3.63)  LDD0171  [1]
DBIA
 Probe Info 
C560(1.18); C571(1.18)  LDD0078  [2]
NAIA_4
 Probe Info 
N.A.  LDD2226  [3]
IPM
 Probe Info 
N.A.  LDD2156  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA DM93 C578(5.93); C75(3.63)  LDD0171  [1]
 LDCM0020  ARS-1620 HCC44 C560(1.18); C571(1.18)  LDD0078  [2]
 LDCM0022  KB02 ICC108 C234(2.17)  LDD2381  [5]
 LDCM0023  KB03 ICC108 C374(2.19); C234(2.60)  LDD2798  [5]
 LDCM0024  KB05 UACC257 C374(2.25)  LDD3325  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Filamin-A (FLNA) Filamin family P21333
Huntingtin (HTT) Huntingtin family P42858

References

1 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
2 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
3 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
4 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
5 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