Details of the Target

General Information of Target

Target ID LDTP00703
Target Name Rho GTPase-activating protein 6 (ARHGAP6)
Gene Name ARHGAP6
Gene ID 395
Synonyms
RHOGAP6; Rho GTPase-activating protein 6; Rho-type GTPase-activating protein 6; Rho-type GTPase-activating protein RhoGAPX-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSAQSLLHSVFSCSSPASSSAASAKGFSKRKLRQTRSLDPALIGGCGSDEAGAEGSARGA
TAGRLYSPSLPAESLGPRLASSSRGPPPRATRLPPPGPLCSSFSTPSTPQEKSPSGSFHF
DYEVPLGRGGLKKSMAWDLPSVLAGPASSRSASSILCSSGGGPNGIFASPRRWLQQRKFQ
SPPDSRGHPYVVWKSEGDFTWNSMSGRSVRLRSVPIQSLSELERARLQEVAFYQLQQDCD
LSCQITIPKDGQKRKKSLRKKLDSLGKEKNKDKEFIPQAFGMPLSQVIANDRAYKLKQDL
QRDEQKDASDFVASLLPFGNKRQNKELSSSNSSLSSTSETPNESTSPNTPEPAPRARRRG
AMSVDSITDLDDNQSRLLEALQLSLPAEAQSKKEKARDKKLSLNPIYRQVPRLVDSCCQH
LEKHGLQTVGIFRVGSSKKRVRQLREEFDRGIDVSLEEEHSVHDVAALLKEFLRDMPDPL
LTRELYTAFINTLLLEPEEQLGTLQLLIYLLPPCNCDTLHRLLQFLSIVARHADDNISKD
GQEVTGNKMTSLNLATIFGPNLLHKQKSSDKEFSVQSSARAEESTAIIAVVQKMIENYEA
LFMVPPDLQNEVLISLLETDPDVVDYLLRRKASQSSSPDMLQSEVSFSVGGRHSSTDSNK
ASSGDISPYDNNSPVLSERSLLAMQEDAAPGGSEKLYRVPGQFMLVGHLSSSKSRESSPG
PRLGKDLSEEPFDIWGTWHSTLKSGSKDPGMTGSSGDIFESSSLRAGPCSLSQGNLSPNW
PRWQGSPAELDSDTQGARRTQAAAPATEGRAHPAVSRACSTPHVQVAGKAERPTARSEQY
LTLSGAHDLSESELDVAGLQSRATPQCQRPHGSGRDDKRPPPPYPGPGKPAAAAAWIQGP
PEGVETPTDQGGQAAEREQQVTQKKLSSANSLPAGEQDSPRLGDAGWLDWQRERWQIWEL
LSTDNPDALPETLV
Target Bioclass
Other
Subcellular location
Cytoplasm
Function
GTPase activator for the Rho-type GTPases by converting them to an inactive GDP-bound state. Could regulate the interactions of signaling molecules with the actin cytoskeleton. Promotes continuous elongation of cytoplasmic processes during cell motility and simultaneous retraction of the cell body changing the cell morphology.
Uniprot ID
O43182
Ensemble ID
ENST00000303025.10
HGNC ID
HGNC:676

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A3KAW SNV: p.E611K .
AN3CA SNV: p.P125S .
DU145 SNV: p.A581V .
HT1080 SNV: p.T963S .
IPC298 SNV: p.P40L .
J82 SNV: p.E221Ter .
MEWO SNV: p.G946C; p.W947C .
MFE319 SNV: p.T345A; p.D535G; p.L613P .
MM1S SNV: p.S655C .
MOLT4 SNV: p.R128H .
NCIH2122 SNV: p.G130S .
NCIH2172 Substitution: p.L764V .
OVK18 SNV: p.S461G .
SW403 SNV: p.R36C .
SW620 SNV: p.S568L .
UACC257 SNV: p.G251R .

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
YN-4
 Probe Info  		100.00  LDD0445  [1]
ONAyne
 Probe Info  		K267(6.25)  LDD0274  [2]
DBIA
 Probe Info  		C819(2.50); C867(1.40)  LDD3335  [3]
YN-1
 Probe Info  		N.A.  LDD0447  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C819(2.06)  LDD2243  [3]
 LDCM0023  KB03 22RV1 C819(1.80)  LDD2660  [3]
 LDCM0024  KB05 MONO-MAC-6 C819(2.50); C867(1.40)  LDD3335  [3]

References

1 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.
2 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
3 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