Details of the Target

General Information of Target

Target ID LDTP09971
Target Name Exostosin-2 (EXT2)
Gene Name EXT2
Gene ID 2132
Synonyms
Exostosin-2; EC 2.4.1.224; Exostosin glycosyltransferase 2; Glucuronosyl-N-acetylglucosaminyl-proteoglycan 4-alpha-N-acetylglucosaminyltransferase; Heparan sulfate co-polymerase subunit EXT1; Multiple exostoses protein 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNNGGKAEKENTPSEANLQEEEVRTLFVSGLPLDIKPRELYLLFRPFKGYEGSLIKLTSK
QPVGFVSFDSRSEAEAAKNALNGIRFDPEIPQTLRLEFAKANTKMAKNKLVGTPNPSTPL
PNTVPQFIAREPYELTVPALYPSSPEVWAPYPLYPAELAPALPPPAFTYPASLHAQMRWL
PPSEATSQGWKSRQFC
Target Bioclass
Enzyme
Family
Glycosyltransferase 47 family
Subcellular location
Endoplasmic reticulum membrane
Function
Glycosyltransferase forming with EXT1 the heterodimeric heparan sulfate polymerase which catalyzes the elongation of the heparan sulfate glycan backbone. Glycan backbone extension consists in the alternating transfer of (1->4)-beta-D-GlcA and (1->4)-alpha-D-GlcNAc residues from their respective UDP-sugar donors. Both EXT1 and EXT2 are required for the full activity of the polymerase since EXT1 bears the N-acetylglucosaminyl-proteoglycan 4-beta-glucuronosyltransferase activity within the complex while EXT2 carries the glucuronosyl-N-acetylglucosaminyl-proteoglycan 4-alpha-N-acetylglucosaminyltransferase activity. Heparan sulfate proteoglycans are ubiquitous components of the extracellular matrix and play an important role in tissue homeostasis and signaling.
Uniprot ID
Q93063
Ensemble ID
ENST00000343631.4
HGNC ID
HGNC:3513

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 SNV: p.A630V .
HT115 SNV: p.F705V .
MEWO SNV: p.P235L .
NCIH661 SNV: p.P503L .
NUGC3 SNV: p.A405V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C184(3.22)  LDD3380  [1]
IPM
 Probe Info  		N.A.  LDD0147  [2]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C280
 Probe Info  		11.88  LDD1950  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C90(1.02)  LDD1507  [4]
 LDCM0215  AC10 HEK-293T C151(1.05); C90(0.96)  LDD1508  [4]
 LDCM0226  AC11 HEK-293T C90(1.04)  LDD1509  [4]
 LDCM0237  AC12 HEK-293T C151(1.01); C90(1.06)  LDD1510  [4]
 LDCM0259  AC14 HEK-293T C151(1.11); C90(0.93)  LDD1512  [4]
 LDCM0270  AC15 HEK-293T C151(0.84); C90(1.13)  LDD1513  [4]
 LDCM0276  AC17 HEK-293T C90(1.02)  LDD1515  [4]
 LDCM0277  AC18 HEK-293T C151(0.89); C90(0.90)  LDD1516  [4]
 LDCM0278  AC19 HEK-293T C90(1.17)  LDD1517  [4]
 LDCM0279  AC2 HEK-293T C151(0.97); C90(0.97)  LDD1518  [4]
 LDCM0280  AC20 HEK-293T C151(1.12); C90(0.98)  LDD1519  [4]
 LDCM0281  AC21 HEK-293T C151(1.02); C90(1.04)  LDD1520  [4]
 LDCM0282  AC22 HEK-293T C151(1.22); C90(0.90)  LDD1521  [4]
 LDCM0283  AC23 HEK-293T C151(0.99); C90(1.02)  LDD1522  [4]
 LDCM0285  AC25 HEK-293T C90(1.05)  LDD1524  [4]
 LDCM0286  AC26 HEK-293T C151(1.02); C90(0.92)  LDD1525  [4]
 LDCM0287  AC27 HEK-293T C90(1.13)  LDD1526  [4]
 LDCM0288  AC28 HEK-293T C151(1.07); C90(1.04)  LDD1527  [4]
 LDCM0289  AC29 HEK-293T C151(1.28); C90(1.07)  LDD1528  [4]
 LDCM0290  AC3 HEK-293T C90(1.04)  LDD1529  [4]
 LDCM0291  AC30 HEK-293T C151(1.01); C90(0.93)  LDD1530  [4]
 LDCM0292  AC31 HEK-293T C151(0.86); C90(0.97)  LDD1531  [4]
 LDCM0294  AC33 HEK-293T C90(0.99)  LDD1533  [4]
 LDCM0295  AC34 HEK-293T C151(0.90); C90(1.01)  LDD1534  [4]
 LDCM0296  AC35 HEK-293T C90(1.01)  LDD1535  [4]
 LDCM0297  AC36 HEK-293T C151(1.09); C90(1.08)  LDD1536  [4]
 LDCM0298  AC37 HEK-293T C151(1.05); C90(1.05)  LDD1537  [4]
 LDCM0299  AC38 HEK-293T C151(0.94); C90(0.94)  LDD1538  [4]
 LDCM0300  AC39 HEK-293T C151(0.94); C90(1.03)  LDD1539  [4]
 LDCM0301  AC4 HEK-293T C151(1.12); C90(0.99)  LDD1540  [4]
 LDCM0303  AC41 HEK-293T C90(1.03)  LDD1542  [4]
 LDCM0304  AC42 HEK-293T C151(1.08); C90(0.98)  LDD1543  [4]
 LDCM0305  AC43 HEK-293T C90(1.02)  LDD1544  [4]
 LDCM0306  AC44 HEK-293T C151(0.99); C90(1.03)  LDD1545  [4]
 LDCM0307  AC45 HEK-293T C151(1.03); C90(1.06)  LDD1546  [4]
 LDCM0308  AC46 HEK-293T C151(1.05); C90(0.94)  LDD1547  [4]
 LDCM0309  AC47 HEK-293T C151(0.94); C90(1.00)  LDD1548  [4]
 LDCM0311  AC49 HEK-293T C90(1.00)  LDD1550  [4]
 LDCM0312  AC5 HEK-293T C151(1.11); C90(1.00)  LDD1551  [4]
 LDCM0313  AC50 HEK-293T C151(1.02); C90(0.97)  LDD1552  [4]
 LDCM0314  AC51 HEK-293T C90(1.03)  LDD1553  [4]
 LDCM0315  AC52 HEK-293T C151(1.09); C90(1.05)  LDD1554  [4]
 LDCM0316  AC53 HEK-293T C151(1.10); C90(1.07)  LDD1555  [4]
 LDCM0317  AC54 HEK-293T C151(1.04); C90(0.95)  LDD1556  [4]
 LDCM0318  AC55 HEK-293T C151(0.86); C90(1.06)  LDD1557  [4]
 LDCM0320  AC57 HEK-293T C90(1.05)  LDD1559  [4]
 LDCM0321  AC58 HEK-293T C151(1.15); C90(0.98)  LDD1560  [4]
 LDCM0322  AC59 HEK-293T C90(1.03)  LDD1561  [4]
 LDCM0323  AC6 HEK-293T C151(1.12); C90(0.93)  LDD1562  [4]
 LDCM0324  AC60 HEK-293T C151(1.09); C90(1.11)  LDD1563  [4]
 LDCM0325  AC61 HEK-293T C151(1.13); C90(1.14)  LDD1564  [4]
 LDCM0326  AC62 HEK-293T C151(1.08); C90(0.93)  LDD1565  [4]
 LDCM0327  AC63 HEK-293T C151(0.87); C90(1.00)  LDD1566  [4]
 LDCM0334  AC7 HEK-293T C151(1.02); C90(0.95)  LDD1568  [4]
 LDCM0248  AKOS034007472 HEK-293T C151(1.13); C90(1.08)  LDD1511  [4]
 LDCM0356  AKOS034007680 HEK-293T C90(0.98)  LDD1570  [4]
 LDCM0368  CL10 HEK-293T C151(1.08); C90(1.06)  LDD1572  [4]
 LDCM0369  CL100 HEK-293T C151(0.91); C90(0.93)  LDD1573  [4]
 LDCM0371  CL102 HEK-293T C151(1.01)  LDD1575  [4]
 LDCM0372  CL103 HEK-293T C90(1.01)  LDD1576  [4]
 LDCM0373  CL104 HEK-293T C151(1.06); C90(0.99)  LDD1577  [4]
 LDCM0375  CL106 HEK-293T C151(1.05)  LDD1579  [4]
 LDCM0376  CL107 HEK-293T C90(0.90)  LDD1580  [4]
 LDCM0377  CL108 HEK-293T C151(0.93); C90(0.87)  LDD1581  [4]
 LDCM0379  CL11 HEK-293T C151(0.99); C90(1.40)  LDD1583  [4]
 LDCM0380  CL110 HEK-293T C151(1.00)  LDD1584  [4]
 LDCM0381  CL111 HEK-293T C90(0.96)  LDD1585  [4]
 LDCM0382  CL112 HEK-293T C151(1.10); C90(0.94)  LDD1586  [4]
 LDCM0384  CL114 HEK-293T C151(1.19)  LDD1588  [4]
 LDCM0385  CL115 HEK-293T C90(1.06)  LDD1589  [4]
 LDCM0386  CL116 HEK-293T C151(1.03); C90(1.00)  LDD1590  [4]
 LDCM0388  CL118 HEK-293T C151(1.22)  LDD1592  [4]
 LDCM0389  CL119 HEK-293T C90(1.13)  LDD1593  [4]
 LDCM0391  CL120 HEK-293T C151(0.93); C90(1.00)  LDD1595  [4]
 LDCM0393  CL122 HEK-293T C151(1.24)  LDD1597  [4]
 LDCM0394  CL123 HEK-293T C90(1.12)  LDD1598  [4]
 LDCM0395  CL124 HEK-293T C151(0.92); C90(0.95)  LDD1599  [4]
 LDCM0397  CL126 HEK-293T C151(1.10)  LDD1601  [4]
 LDCM0398  CL127 HEK-293T C90(0.98)  LDD1602  [4]
 LDCM0399  CL128 HEK-293T C151(0.93); C90(0.91)  LDD1603  [4]
 LDCM0401  CL14 HEK-293T C151(1.18)  LDD1605  [4]
 LDCM0402  CL15 HEK-293T C90(1.12)  LDD1606  [4]
 LDCM0403  CL16 HEK-293T C151(1.20); C90(1.05)  LDD1607  [4]
 LDCM0404  CL17 HEK-293T C90(1.12)  LDD1608  [4]
 LDCM0405  CL18 HEK-293T C151(0.95); C90(1.15)  LDD1609  [4]
 LDCM0406  CL19 HEK-293T C90(1.01)  LDD1610  [4]
 LDCM0407  CL2 HEK-293T C151(1.23)  LDD1611  [4]
 LDCM0408  CL20 HEK-293T C151(1.25); C90(1.07)  LDD1612  [4]
 LDCM0409  CL21 HEK-293T C151(1.25); C90(1.16)  LDD1613  [4]
 LDCM0410  CL22 HEK-293T C151(1.07); C90(1.04)  LDD1614  [4]
 LDCM0411  CL23 HEK-293T C151(1.01); C90(1.40)  LDD1615  [4]
 LDCM0414  CL26 HEK-293T C151(1.15)  LDD1618  [4]
 LDCM0415  CL27 HEK-293T C90(0.95)  LDD1619  [4]
 LDCM0416  CL28 HEK-293T C151(1.04); C90(1.00)  LDD1620  [4]
 LDCM0417  CL29 HEK-293T C90(0.99)  LDD1621  [4]
 LDCM0418  CL3 HEK-293T C90(1.03)  LDD1622  [4]
 LDCM0419  CL30 HEK-293T C151(0.98); C90(1.05)  LDD1623  [4]
 LDCM0420  CL31 HEK-293T C90(1.14)  LDD1624  [4]
 LDCM0421  CL32 HEK-293T C151(0.99); C90(1.06)  LDD1625  [4]
 LDCM0422  CL33 HEK-293T C151(1.25); C90(1.21)  LDD1626  [4]
 LDCM0423  CL34 HEK-293T C151(1.03); C90(1.14)  LDD1627  [4]
 LDCM0424  CL35 HEK-293T C151(1.09); C90(1.39)  LDD1628  [4]
 LDCM0428  CL39 HEK-293T C90(1.08)  LDD1632  [4]
 LDCM0429  CL4 HEK-293T C151(0.93); C90(1.18)  LDD1633  [4]
 LDCM0430  CL40 HEK-293T C151(0.96); C90(0.98)  LDD1634  [4]
 LDCM0431  CL41 HEK-293T C90(0.95)  LDD1635  [4]
 LDCM0432  CL42 HEK-293T C151(0.95); C90(1.01)  LDD1636  [4]
 LDCM0433  CL43 HEK-293T C90(1.13)  LDD1637  [4]
 LDCM0434  CL44 HEK-293T C151(0.96); C90(1.14)  LDD1638  [4]
 LDCM0435  CL45 HEK-293T C151(1.45); C90(1.07)  LDD1639  [4]
 LDCM0436  CL46 HEK-293T C151(1.02); C90(0.91)  LDD1640  [4]
 LDCM0437  CL47 HEK-293T C151(0.89); C90(1.24)  LDD1641  [4]
 LDCM0440  CL5 HEK-293T C90(1.07)  LDD1644  [4]
 LDCM0441  CL50 HEK-293T C151(1.13)  LDD1645  [4]
 LDCM0443  CL52 HEK-293T C151(1.10); C90(1.06)  LDD1646  [4]
 LDCM0444  CL53 HEK-293T C90(1.17)  LDD1647  [4]
 LDCM0445  CL54 HEK-293T C151(1.20); C90(1.25)  LDD1648  [4]
 LDCM0446  CL55 HEK-293T C90(1.09)  LDD1649  [4]
 LDCM0447  CL56 HEK-293T C151(1.12); C90(1.08)  LDD1650  [4]
 LDCM0448  CL57 HEK-293T C151(1.29); C90(1.22)  LDD1651  [4]
 LDCM0449  CL58 HEK-293T C151(1.30); C90(1.01)  LDD1652  [4]
 LDCM0450  CL59 HEK-293T C151(1.13); C90(1.37)  LDD1653  [4]
 LDCM0451  CL6 HEK-293T C151(1.06); C90(1.11)  LDD1654  [4]
 LDCM0454  CL62 HEK-293T C151(1.38)  LDD1657  [4]
 LDCM0455  CL63 HEK-293T C90(1.00)  LDD1658  [4]
 LDCM0456  CL64 HEK-293T C151(0.95); C90(1.08)  LDD1659  [4]
 LDCM0457  CL65 HEK-293T C90(1.00)  LDD1660  [4]
 LDCM0458  CL66 HEK-293T C151(1.19); C90(1.06)  LDD1661  [4]
 LDCM0459  CL67 HEK-293T C90(1.17)  LDD1662  [4]
 LDCM0460  CL68 HEK-293T C151(1.32); C90(1.22)  LDD1663  [4]
 LDCM0461  CL69 HEK-293T C151(1.39); C90(1.22)  LDD1664  [4]
 LDCM0462  CL7 HEK-293T C90(1.14)  LDD1665  [4]
 LDCM0463  CL70 HEK-293T C151(1.02); C90(0.98)  LDD1666  [4]
 LDCM0464  CL71 HEK-293T C151(1.19); C90(1.30)  LDD1667  [4]
 LDCM0467  CL74 HEK-293T C151(1.17)  LDD1670  [4]
 LDCM0469  CL76 HEK-293T C151(1.09); C90(1.00)  LDD1672  [4]
 LDCM0470  CL77 HEK-293T C90(1.02)  LDD1673  [4]
 LDCM0471  CL78 HEK-293T C151(0.89); C90(1.03)  LDD1674  [4]
 LDCM0472  CL79 HEK-293T C90(1.13)  LDD1675  [4]
 LDCM0473  CL8 HEK-293T C151(1.18); C90(1.29)  LDD1676  [4]
 LDCM0474  CL80 HEK-293T C151(0.97); C90(1.09)  LDD1677  [4]
 LDCM0475  CL81 HEK-293T C151(1.30); C90(1.20)  LDD1678  [4]
 LDCM0476  CL82 HEK-293T C151(1.11); C90(1.16)  LDD1679  [4]
 LDCM0477  CL83 HEK-293T C151(0.99); C90(1.29)  LDD1680  [4]
 LDCM0480  CL86 HEK-293T C151(1.04)  LDD1683  [4]
 LDCM0481  CL87 HEK-293T C90(0.94)  LDD1684  [4]
 LDCM0482  CL88 HEK-293T C151(0.86); C90(1.04)  LDD1685  [4]
 LDCM0483  CL89 HEK-293T C90(1.03)  LDD1686  [4]
 LDCM0484  CL9 HEK-293T C151(1.41); C90(1.07)  LDD1687  [4]
 LDCM0485  CL90 HEK-293T C151(1.14); C90(1.33)  LDD1688  [4]
 LDCM0486  CL91 HEK-293T C90(1.13)  LDD1689  [4]
 LDCM0487  CL92 HEK-293T C151(1.21); C90(1.16)  LDD1690  [4]
 LDCM0488  CL93 HEK-293T C151(1.26); C90(1.19)  LDD1691  [4]
 LDCM0489  CL94 HEK-293T C151(1.02); C90(1.07)  LDD1692  [4]
 LDCM0490  CL95 HEK-293T C151(0.72); C90(1.43)  LDD1693  [4]
 LDCM0493  CL98 HEK-293T C151(0.85)  LDD1696  [4]
 LDCM0494  CL99 HEK-293T C90(1.01)  LDD1697  [4]
 LDCM0495  E2913 HEK-293T C90(1.07)  LDD1698  [4]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C90(2.67); C96(1.94)  LDD1702  [5]
 LDCM0468  Fragment33 HEK-293T C90(1.03)  LDD1671  [4]
 LDCM0427  Fragment51 HEK-293T C151(1.03)  LDD1631  [4]
 LDCM0022  KB02 A2780 C184(2.26)  LDD2254  [1]
 LDCM0023  KB03 MDA-MB-231 C96(8.04)  LDD1701  [5]
 LDCM0024  KB05 OV-90 C184(3.22)  LDD3380  [1]

References

1 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
2 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
3 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
4 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
5 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761