Details of the Target

General Information of Target

Target ID LDTP10876
Target Name Arf-GAP with GTPase, ANK repeat and PH domain-containing protein 2 (AGAP2)
Gene Name AGAP2
Gene ID 116986
Synonyms
CENTG1; KIAA0167; Arf-GAP with GTPase, ANK repeat and PH domain-containing protein 2; AGAP-2; Centaurin-gamma-1; Cnt-g1; GTP-binding and GTPase-activating protein 2; GGAP2; Phosphatidylinositol 3-kinase enhancer; PIKE
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDTARIAVVGAGVVGLSTAVCISKLVPRCSVTIISDKFTPDTTSDVAAGMLIPHTYPDTP
IHTQKQWFRETFNHLFAIANSAEAGDAGVHLVSGWQIFQSTPTEEVPFWADVVLGFRKMT
EAELKKFPQYVFGQAFTTLKCECPAYLPWLEKRIKGSGGWTLTRRIEDLWELHPSFDIVV
NCSGLGSRQLAGDSKIFPVRGQVLQVQAPWVEHFIRDGSGLTYIYPGTSHVTLGGTRQKG
DWNLSPDAENSREILSRCCALEPSLHGACNIREKVGLRPYRPGVRLQTELLARDGQRLPV
VHHYGHGSGGISVHWGTALEAARLVSECVHALRTPIPKSNL
Target Bioclass
Other
Family
Centaurin gamma-like family
Subcellular location
Cytoplasm
Function
GTPase-activating protein (GAP) for ARF1 and ARF5, which also shows strong GTPase activity. Isoform 1 participates in the prevention of neuronal apoptosis by enhancing PI3 kinase activity. It aids the coupling of metabotropic glutamate receptor 1 (GRM1) to cytoplasmic PI3 kinase by interacting with Homer scaffolding proteins, and also seems to mediate anti-apoptotic effects of NGF by activating nuclear PI3 kinase. Isoform 2 does not stimulate PI3 kinase but may protect cells from apoptosis by stimulating Akt. It also regulates the adapter protein 1 (AP-1)-dependent trafficking of proteins in the endosomal system. It seems to be oncogenic. It is overexpressed in cancer cells, prevents apoptosis and promotes cancer cell invasion.
Uniprot ID
Q99490
Ensemble ID
ENST00000257897.7
HGNC ID
HGNC:16921

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K734(5.88)  LDD0277  [1]
DBIA
 Probe Info  		C1139(0.94); C1148(0.94)  LDD0532  [2]
4-Iodoacetamidophenylacetylene
 Probe Info  		C579(0.00); C811(0.00)  LDD0038  [3]
IA-alkyne
 Probe Info  		C579(0.00); C536(0.00)  LDD0036  [3]
Lodoacetamide azide
 Probe Info  		C811(0.00); C579(0.00); C536(0.00)  LDD0037  [3]
NAIA_4
 Probe Info  		N.A.  LDD2226  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HCT 116 C1139(0.94); C1148(0.94)  LDD0532  [2]
 LDCM0216  AC100 HCT 116 C542(1.21); C548(1.21)  LDD0533  [2]
 LDCM0217  AC101 HCT 116 C542(0.82); C548(0.82)  LDD0534  [2]
 LDCM0218  AC102 HCT 116 C542(1.51); C548(1.51)  LDD0535  [2]
 LDCM0219  AC103 HCT 116 C542(1.65); C548(1.65)  LDD0536  [2]
 LDCM0220  AC104 HCT 116 C542(1.34); C548(1.34)  LDD0537  [2]
 LDCM0221  AC105 HCT 116 C542(1.19); C548(1.19)  LDD0538  [2]
 LDCM0222  AC106 HCT 116 C542(1.22); C548(1.22)  LDD0539  [2]
 LDCM0223  AC107 HCT 116 C542(1.02); C548(1.02)  LDD0540  [2]
 LDCM0224  AC108 HCT 116 C542(1.55); C548(1.55)  LDD0541  [2]
 LDCM0225  AC109 HCT 116 C542(1.49); C548(1.49)  LDD0542  [2]
 LDCM0226  AC11 HCT 116 C1139(0.88); C1148(0.88)  LDD0543  [2]
 LDCM0227  AC110 HCT 116 C542(1.15); C548(1.15)  LDD0544  [2]
 LDCM0228  AC111 HCT 116 C542(1.52); C548(1.52)  LDD0545  [2]
 LDCM0229  AC112 HCT 116 C542(1.13); C548(1.13)  LDD0546  [2]
 LDCM0237  AC12 HCT 116 C1139(0.79); C1148(0.79)  LDD0554  [2]
 LDCM0246  AC128 HCT 116 C1139(0.58); C1148(0.58)  LDD0563  [2]
 LDCM0247  AC129 HCT 116 C1139(0.31); C1148(0.31)  LDD0564  [2]
 LDCM0249  AC130 HCT 116 C1139(0.36); C1148(0.36)  LDD0566  [2]
 LDCM0250  AC131 HCT 116 C1139(0.61); C1148(0.61)  LDD0567  [2]
 LDCM0251  AC132 HCT 116 C1139(0.30); C1148(0.30)  LDD0568  [2]
 LDCM0252  AC133 HCT 116 C1139(0.44); C1148(0.44)  LDD0569  [2]
 LDCM0253  AC134 HCT 116 C1139(0.57); C1148(0.57)  LDD0570  [2]
 LDCM0254  AC135 HCT 116 C1139(0.60); C1148(0.60)  LDD0571  [2]
 LDCM0255  AC136 HCT 116 C1139(0.43); C1148(0.43)  LDD0572  [2]
 LDCM0256  AC137 HCT 116 C1139(0.50); C1148(0.50)  LDD0573  [2]
 LDCM0257  AC138 HCT 116 C1139(0.47); C1148(0.47)  LDD0574  [2]
 LDCM0258  AC139 HCT 116 C1139(0.38); C1148(0.38)  LDD0575  [2]
 LDCM0259  AC14 HCT 116 C1139(0.80); C1148(0.80)  LDD0576  [2]
 LDCM0260  AC140 HCT 116 C1139(0.36); C1148(0.36)  LDD0577  [2]
 LDCM0261  AC141 HCT 116 C1139(0.53); C1148(0.53)  LDD0578  [2]
 LDCM0262  AC142 HCT 116 C1139(0.37); C1148(0.37)  LDD0579  [2]
 LDCM0263  AC143 HCT 116 C542(1.21); C548(1.21)  LDD0580  [2]
 LDCM0264  AC144 HCT 116 C542(0.88); C548(0.88)  LDD0581  [2]
 LDCM0265  AC145 HCT 116 C542(1.12); C548(1.12)  LDD0582  [2]
 LDCM0266  AC146 HCT 116 C542(1.16); C548(1.16)  LDD0583  [2]
 LDCM0267  AC147 HCT 116 C542(1.15); C548(1.15)  LDD0584  [2]
 LDCM0268  AC148 HCT 116 C542(1.33); C548(1.33)  LDD0585  [2]
 LDCM0269  AC149 HCT 116 C542(1.05); C548(1.05)  LDD0586  [2]
 LDCM0270  AC15 HCT 116 C1139(1.05); C1148(1.05)  LDD0587  [2]
 LDCM0271  AC150 HCT 116 C542(0.59); C548(0.59)  LDD0588  [2]
 LDCM0272  AC151 HCT 116 C542(0.94); C548(0.94)  LDD0589  [2]
 LDCM0273  AC152 HCT 116 C542(1.62); C548(1.62)  LDD0590  [2]
 LDCM0274  AC153 HCT 116 C542(1.05); C548(1.05)  LDD0591  [2]
 LDCM0621  AC154 HCT 116 C542(1.20); C548(1.20)  LDD2158  [2]
 LDCM0622  AC155 HCT 116 C542(1.18); C548(1.18)  LDD2159  [2]
 LDCM0623  AC156 HCT 116 C542(0.94); C548(0.94)  LDD2160  [2]
 LDCM0624  AC157 HCT 116 C542(1.05); C548(1.05)  LDD2161  [2]
 LDCM0308  AC46 HCT 116 C542(1.21); C548(1.21)  LDD0625  [2]
 LDCM0309  AC47 HCT 116 C542(0.91); C548(0.91)  LDD0626  [2]
 LDCM0310  AC48 HCT 116 C542(0.81); C548(0.81)  LDD0627  [2]
 LDCM0311  AC49 HCT 116 C542(0.86); C548(0.86)  LDD0628  [2]
 LDCM0313  AC50 HCT 116 C542(0.89); C548(0.89)  LDD0630  [2]
 LDCM0314  AC51 HCT 116 C542(1.12); C548(1.12)  LDD0631  [2]
 LDCM0315  AC52 HCT 116 C542(0.74); C548(0.74)  LDD0632  [2]
 LDCM0316  AC53 HCT 116 C542(0.81); C548(0.81)  LDD0633  [2]
 LDCM0317  AC54 HCT 116 C542(0.69); C548(0.69)  LDD0634  [2]
 LDCM0318  AC55 HCT 116 C542(0.81); C548(0.81)  LDD0635  [2]
 LDCM0319  AC56 HCT 116 C542(1.18); C548(1.18)  LDD0636  [2]
 LDCM0323  AC6 HCT 116 C1139(1.01); C1148(1.01)  LDD0640  [2]
 LDCM0332  AC68 HCT 116 C542(0.97); C548(0.97)  LDD0649  [2]
 LDCM0333  AC69 HCT 116 C542(1.13); C548(1.13)  LDD0650  [2]
 LDCM0334  AC7 HCT 116 C1139(0.67); C1148(0.67)  LDD0651  [2]
 LDCM0335  AC70 HCT 116 C542(0.90); C548(0.90)  LDD0652  [2]
 LDCM0336  AC71 HCT 116 C542(0.91); C548(0.91)  LDD0653  [2]
 LDCM0337  AC72 HCT 116 C542(1.13); C548(1.13)  LDD0654  [2]
 LDCM0338  AC73 HCT 116 C542(1.28); C548(1.28)  LDD0655  [2]
 LDCM0339  AC74 HCT 116 C542(1.27); C548(1.27)  LDD0656  [2]
 LDCM0340  AC75 HCT 116 C542(1.06); C548(1.06)  LDD0657  [2]
 LDCM0341  AC76 HCT 116 C542(1.24); C548(1.24)  LDD0658  [2]
 LDCM0342  AC77 HCT 116 C542(1.22); C548(1.22)  LDD0659  [2]
 LDCM0343  AC78 HCT 116 C542(1.01); C548(1.01)  LDD0660  [2]
 LDCM0344  AC79 HCT 116 C542(0.93); C548(0.93)  LDD0661  [2]
 LDCM0345  AC8 HCT 116 C1139(0.78); C1148(0.78)  LDD0662  [2]
 LDCM0346  AC80 HCT 116 C542(1.12); C548(1.12)  LDD0663  [2]
 LDCM0347  AC81 HCT 116 C542(0.80); C548(0.80)  LDD0664  [2]
 LDCM0348  AC82 HCT 116 C542(0.93); C548(0.93)  LDD0665  [2]
 LDCM0365  AC98 HCT 116 C542(1.60); C548(1.60)  LDD0682  [2]
 LDCM0366  AC99 HCT 116 C542(1.22); C548(1.22)  LDD0683  [2]
 LDCM0248  AKOS034007472 HCT 116 C1139(1.07); C1148(1.07)  LDD0565  [2]
 LDCM0356  AKOS034007680 HCT 116 C1139(0.73); C1148(0.73)  LDD0673  [2]
 LDCM0275  AKOS034007705 HCT 116 C1139(0.95); C1148(0.95)  LDD0592  [2]
 LDCM0370  CL101 HCT 116 C1139(0.82); C1148(0.82)  LDD0687  [2]
 LDCM0371  CL102 HCT 116 C1139(0.84); C1148(0.84)  LDD0688  [2]
 LDCM0372  CL103 HCT 116 C1139(0.83); C1148(0.83)  LDD0689  [2]
 LDCM0373  CL104 HCT 116 C1139(1.28); C1148(1.28)  LDD0690  [2]
 LDCM0392  CL121 HCT 116 C542(1.83); C548(1.83)  LDD0709  [2]
 LDCM0393  CL122 HCT 116 C542(0.96); C548(0.96)  LDD0710  [2]
 LDCM0394  CL123 HCT 116 C542(1.74); C548(1.74)  LDD0711  [2]
 LDCM0395  CL124 HCT 116 C542(1.18); C548(1.18)  LDD0712  [2]
 LDCM0403  CL16 HCT 116 C1139(0.74); C1148(0.74)  LDD0720  [2]
 LDCM0404  CL17 HCT 116 C1139(0.90); C1148(0.90)  LDD0721  [2]
 LDCM0405  CL18 HCT 116 C1139(0.72); C1148(0.72)  LDD0722  [2]
 LDCM0406  CL19 HCT 116 C1139(0.84); C1148(0.84)  LDD0723  [2]
 LDCM0408  CL20 HCT 116 C1139(0.89); C1148(0.89)  LDD0725  [2]
 LDCM0409  CL21 HCT 116 C1139(0.83); C1148(0.83)  LDD0726  [2]
 LDCM0410  CL22 HCT 116 C1139(0.81); C1148(0.81)  LDD0727  [2]
 LDCM0411  CL23 HCT 116 C1139(0.87); C1148(0.87)  LDD0728  [2]
 LDCM0412  CL24 HCT 116 C1139(0.82); C1148(0.82)  LDD0729  [2]
 LDCM0413  CL25 HCT 116 C1139(0.69); C1148(0.69)  LDD0730  [2]
 LDCM0414  CL26 HCT 116 C1139(0.81); C1148(0.81)  LDD0731  [2]
 LDCM0415  CL27 HCT 116 C1139(0.79); C1148(0.79)  LDD0732  [2]
 LDCM0416  CL28 HCT 116 C1139(0.70); C1148(0.70)  LDD0733  [2]
 LDCM0417  CL29 HCT 116 C1139(0.72); C1148(0.72)  LDD0734  [2]
 LDCM0419  CL30 HCT 116 C1139(0.82); C1148(0.82)  LDD0736  [2]
 LDCM0436  CL46 HCT 116 C1139(1.42); C1148(1.42)  LDD0753  [2]
 LDCM0437  CL47 HCT 116 C1139(2.06); C1148(2.06)  LDD0754  [2]
 LDCM0438  CL48 HCT 116 C1139(1.29); C1148(1.29)  LDD0755  [2]
 LDCM0439  CL49 HCT 116 C1139(1.34); C1148(1.34)  LDD0756  [2]
 LDCM0441  CL50 HCT 116 C1139(1.39); C1148(1.39)  LDD0758  [2]
 LDCM0442  CL51 HCT 116 C1139(1.23); C1148(1.23)  LDD0759  [2]
 LDCM0443  CL52 HCT 116 C1139(1.07); C1148(1.07)  LDD0760  [2]
 LDCM0444  CL53 HCT 116 C1139(1.65); C1148(1.65)  LDD0761  [2]
 LDCM0445  CL54 HCT 116 C1139(1.68); C1148(1.68)  LDD0762  [2]
 LDCM0446  CL55 HCT 116 C1139(1.99); C1148(1.99)  LDD0763  [2]
 LDCM0447  CL56 HCT 116 C1139(1.02); C1148(1.02)  LDD0764  [2]
 LDCM0448  CL57 HCT 116 C1139(1.04); C1148(1.04)  LDD0765  [2]
 LDCM0449  CL58 HCT 116 C1139(1.58); C1148(1.58)  LDD0766  [2]
 LDCM0450  CL59 HCT 116 C1139(1.31); C1148(1.31)  LDD0767  [2]
 LDCM0452  CL60 HCT 116 C1139(1.17); C1148(1.17)  LDD0769  [2]
 LDCM0453  CL61 HCT 116 C1139(0.89); C1148(0.89)  LDD0770  [2]
 LDCM0454  CL62 HCT 116 C1139(1.19); C1148(1.19)  LDD0771  [2]
 LDCM0455  CL63 HCT 116 C1139(0.67); C1148(0.67)  LDD0772  [2]
 LDCM0456  CL64 HCT 116 C1139(0.78); C1148(0.78)  LDD0773  [2]
 LDCM0457  CL65 HCT 116 C1139(0.75); C1148(0.75)  LDD0774  [2]
 LDCM0458  CL66 HCT 116 C1139(0.63); C1148(0.63)  LDD0775  [2]
 LDCM0459  CL67 HCT 116 C1139(0.92); C1148(0.92)  LDD0776  [2]
 LDCM0460  CL68 HCT 116 C1139(0.53); C1148(0.53)  LDD0777  [2]
 LDCM0461  CL69 HCT 116 C1139(0.94); C1148(0.94)  LDD0778  [2]
 LDCM0463  CL70 HCT 116 C1139(0.61); C1148(0.61)  LDD0780  [2]
 LDCM0464  CL71 HCT 116 C1139(0.57); C1148(0.57)  LDD0781  [2]
 LDCM0465  CL72 HCT 116 C1139(0.82); C1148(0.82)  LDD0782  [2]
 LDCM0466  CL73 HCT 116 C1139(0.80); C1148(0.80)  LDD0783  [2]
 LDCM0467  CL74 HCT 116 C1139(0.64); C1148(0.64)  LDD0784  [2]
 LDCM0625  F8 Ramos C811(1.13)  LDD2187  [5]
 LDCM0572  Fragment10 Ramos C811(1.06)  LDD2189  [5]
 LDCM0573  Fragment11 Ramos C811(2.25)  LDD2190  [5]
 LDCM0574  Fragment12 Ramos C811(0.80)  LDD2191  [5]
 LDCM0575  Fragment13 Ramos C811(1.00)  LDD2192  [5]
 LDCM0576  Fragment14 Ramos C811(0.92)  LDD2193  [5]
 LDCM0579  Fragment20 Ramos C811(0.80)  LDD2194  [5]
 LDCM0580  Fragment21 Ramos C811(1.07)  LDD2195  [5]
 LDCM0582  Fragment23 Ramos C811(1.18)  LDD2196  [5]
 LDCM0578  Fragment27 Ramos C811(1.14)  LDD2197  [5]
 LDCM0586  Fragment28 Ramos C811(0.58)  LDD2198  [5]
 LDCM0588  Fragment30 Ramos C811(1.21)  LDD2199  [5]
 LDCM0589  Fragment31 Ramos C811(0.90)  LDD2200  [5]
 LDCM0590  Fragment32 Ramos C811(1.00)  LDD2201  [5]
 LDCM0468  Fragment33 HCT 116 C1139(0.86); C1148(0.86)  LDD0785  [2]
 LDCM0596  Fragment38 Ramos C811(0.95)  LDD2203  [5]
 LDCM0566  Fragment4 Ramos C811(0.77)  LDD2184  [5]
 LDCM0610  Fragment52 Ramos C811(1.27)  LDD2204  [5]
 LDCM0614  Fragment56 Ramos C811(1.03)  LDD2205  [5]
 LDCM0569  Fragment7 Ramos C811(0.91)  LDD2186  [5]
 LDCM0571  Fragment9 Ramos C811(0.93)  LDD2188  [5]
 LDCM0022  KB02 T cell C915(7.22); C916(0.00)  LDD1703  [6]
 LDCM0023  KB03 Ramos C811(0.86)  LDD2183  [5]
 LDCM0024  KB05 MOLM-16 C536(2.08)  LDD3334  [7]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Insulin receptor (INSR) Tyr protein kinase family P06213
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Signal transducer and activator of transcription 5A (STAT5A) Transcription factor STAT family P42229

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 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 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
4 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
5 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
6 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
7 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