Details of the Target

General Information of Target

Target ID LDTP06531
Target Name Exostosin-1 (EXT1)
Gene Name EXT1
Gene ID 2131
Synonyms
Exostosin-1; EC 2.4.1.225; Exostosin glycosyltransferase 1; Heparan sulfate co-polymerase subunit EXT1; Multiple exostoses protein 1; N-acetylglucosaminyl-proteoglycan 4-beta-glucuronosyltransferase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQAKKRYFILLSAGSCLALLFYFGGLQFRASRSHSRREEHSGRNGLHHPSPDHFWPRFPD
ALRPFVPWDQLENEDSSVHISPRQKRDANSSIYKGKKCRMESCFDFTLCKKNGFKVYVYP
QQKGEKIAESYQNILAAIEGSRFYTSDPSQACLFVLSLDTLDRDQLSPQYVHNLRSKVQS
LHLWNNGRNHLIFNLYSGTWPDYTEDVGFDIGQAMLAKASISTENFRPNFDVSIPLFSKD
HPRTGGERGFLKFNTIPPLRKYMLVFKGKRYLTGIGSDTRNALYHVHNGEDVVLLTTCKH
GKDWQKHKDSRCDRDNTEYEKYDYREMLHNATFCLVPRGRRLGSFRFLEALQAACVPVML
SNGWELPFSEVINWNQAAVIGDERLLLQIPSTIRSIHQDKILALRQQTQFLWEAYFSSVE
KIVLTTLEIIQDRIFKHISRNSLIWNKHPGGLFVLPQYSSYLGDFPYYYANLGLKPPSKF
TAVIHAVTPLVSQSQPVLKLLVAAAKSQYCAQIIVLWNCDKPLPAKHRWPATAVPVVVIE
GESKVMSSRFLPYDNIITDAVLSLDEDTVLSTTEVDFAFTVWQSFPERIVGYPARSHFWD
NSKERWGYTSKWTNDYSMVLTGAAIYHKYYHYLYSHYLPASLKNMVDQLANCEDILMNFL
VSAVTKLPPIKVTQKKQYKETMMGQTSRASRWADPDHFAQRQSCMNTFASWFGYMPLIHS
QMRLDPVLFKDQVSILRKKYRDIERL
Target Bioclass
Enzyme
Family
Glycosyltransferase 47 family
Subcellular location
Endoplasmic reticulum membrane
Function
Glycosyltransferase forming with EXT2 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
Q16394
Ensemble ID
ENST00000378204.7
HGNC ID
HGNC:3512

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C312(0.96)  LDD1492  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C312(1.03)  LDD1508  [1]
 LDCM0226  AC11 HEK-293T C312(1.23)  LDD1509  [1]
 LDCM0259  AC14 HEK-293T C312(1.11)  LDD1512  [1]
 LDCM0270  AC15 HEK-293T C312(1.19)  LDD1513  [1]
 LDCM0277  AC18 HEK-293T C312(1.05)  LDD1516  [1]
 LDCM0278  AC19 HEK-293T C312(1.56)  LDD1517  [1]
 LDCM0279  AC2 HEK-293T C312(1.11)  LDD1518  [1]
 LDCM0282  AC22 HEK-293T C312(0.90)  LDD1521  [1]
 LDCM0283  AC23 HEK-293T C312(1.08)  LDD1522  [1]
 LDCM0286  AC26 HEK-293T C312(1.04)  LDD1525  [1]
 LDCM0287  AC27 HEK-293T C312(1.15)  LDD1526  [1]
 LDCM0290  AC3 HEK-293T C312(1.19)  LDD1529  [1]
 LDCM0291  AC30 HEK-293T C312(0.99)  LDD1530  [1]
 LDCM0292  AC31 HEK-293T C312(1.02)  LDD1531  [1]
 LDCM0295  AC34 HEK-293T C312(1.09)  LDD1534  [1]
 LDCM0296  AC35 HEK-293T C312(1.13)  LDD1535  [1]
 LDCM0299  AC38 HEK-293T C312(1.04)  LDD1538  [1]
 LDCM0300  AC39 HEK-293T C312(1.07)  LDD1539  [1]
 LDCM0304  AC42 HEK-293T C312(1.12)  LDD1543  [1]
 LDCM0305  AC43 HEK-293T C312(1.05)  LDD1544  [1]
 LDCM0308  AC46 HEK-293T C312(1.34)  LDD1547  [1]
 LDCM0309  AC47 HEK-293T C312(1.20)  LDD1548  [1]
 LDCM0313  AC50 HEK-293T C312(1.12)  LDD1552  [1]
 LDCM0314  AC51 HEK-293T C312(1.15)  LDD1553  [1]
 LDCM0317  AC54 HEK-293T C312(1.12)  LDD1556  [1]
 LDCM0318  AC55 HEK-293T C312(1.18)  LDD1557  [1]
 LDCM0321  AC58 HEK-293T C312(1.11)  LDD1560  [1]
 LDCM0322  AC59 HEK-293T C312(1.22)  LDD1561  [1]
 LDCM0323  AC6 HEK-293T C312(1.11)  LDD1562  [1]
 LDCM0326  AC62 HEK-293T C312(1.09)  LDD1565  [1]
 LDCM0327  AC63 HEK-293T C312(1.12)  LDD1566  [1]
 LDCM0334  AC7 HEK-293T C312(1.13)  LDD1568  [1]
 LDCM0368  CL10 HEK-293T C312(0.76)  LDD1572  [1]
 LDCM0369  CL100 HEK-293T C312(0.99)  LDD1573  [1]
 LDCM0373  CL104 HEK-293T C312(1.04)  LDD1577  [1]
 LDCM0377  CL108 HEK-293T C312(1.10)  LDD1581  [1]
 LDCM0379  CL11 HEK-293T C312(0.90)  LDD1583  [1]
 LDCM0382  CL112 HEK-293T C312(1.22)  LDD1586  [1]
 LDCM0386  CL116 HEK-293T C312(1.15)  LDD1590  [1]
 LDCM0391  CL120 HEK-293T C312(1.03)  LDD1595  [1]
 LDCM0395  CL124 HEK-293T C312(1.31)  LDD1599  [1]
 LDCM0399  CL128 HEK-293T C312(1.11)  LDD1603  [1]
 LDCM0403  CL16 HEK-293T C312(0.94)  LDD1607  [1]
 LDCM0405  CL18 HEK-293T C312(1.01)  LDD1609  [1]
 LDCM0406  CL19 HEK-293T C312(0.98)  LDD1610  [1]
 LDCM0410  CL22 HEK-293T C312(0.85)  LDD1614  [1]
 LDCM0411  CL23 HEK-293T C312(0.89)  LDD1615  [1]
 LDCM0416  CL28 HEK-293T C312(1.14)  LDD1620  [1]
 LDCM0419  CL30 HEK-293T C312(1.03)  LDD1623  [1]
 LDCM0420  CL31 HEK-293T C312(1.03)  LDD1624  [1]
 LDCM0423  CL34 HEK-293T C312(0.99)  LDD1627  [1]
 LDCM0424  CL35 HEK-293T C312(0.94)  LDD1628  [1]
 LDCM0429  CL4 HEK-293T C312(0.95)  LDD1633  [1]
 LDCM0430  CL40 HEK-293T C312(0.98)  LDD1634  [1]
 LDCM0432  CL42 HEK-293T C312(0.96)  LDD1636  [1]
 LDCM0433  CL43 HEK-293T C312(0.96)  LDD1637  [1]
 LDCM0436  CL46 HEK-293T C312(0.88)  LDD1640  [1]
 LDCM0437  CL47 HEK-293T C312(0.85)  LDD1641  [1]
 LDCM0443  CL52 HEK-293T C312(1.11)  LDD1646  [1]
 LDCM0445  CL54 HEK-293T C312(1.04)  LDD1648  [1]
 LDCM0446  CL55 HEK-293T C312(0.89)  LDD1649  [1]
 LDCM0449  CL58 HEK-293T C312(0.99)  LDD1652  [1]
 LDCM0450  CL59 HEK-293T C312(0.99)  LDD1653  [1]
 LDCM0451  CL6 HEK-293T C312(1.03)  LDD1654  [1]
 LDCM0456  CL64 HEK-293T C312(0.95)  LDD1659  [1]
 LDCM0458  CL66 HEK-293T C312(0.98)  LDD1661  [1]
 LDCM0459  CL67 HEK-293T C312(0.96)  LDD1662  [1]
 LDCM0462  CL7 HEK-293T C312(0.97)  LDD1665  [1]
 LDCM0463  CL70 HEK-293T C312(0.99)  LDD1666  [1]
 LDCM0464  CL71 HEK-293T C312(1.02)  LDD1667  [1]
 LDCM0469  CL76 HEK-293T C312(1.10)  LDD1672  [1]
 LDCM0471  CL78 HEK-293T C312(1.18)  LDD1674  [1]
 LDCM0472  CL79 HEK-293T C312(1.00)  LDD1675  [1]
 LDCM0476  CL82 HEK-293T C312(1.06)  LDD1679  [1]
 LDCM0477  CL83 HEK-293T C312(0.98)  LDD1680  [1]
 LDCM0482  CL88 HEK-293T C312(1.17)  LDD1685  [1]
 LDCM0485  CL90 HEK-293T C312(1.32)  LDD1688  [1]
 LDCM0486  CL91 HEK-293T C312(1.07)  LDD1689  [1]
 LDCM0489  CL94 HEK-293T C312(1.01)  LDD1692  [1]
 LDCM0490  CL95 HEK-293T C312(1.08)  LDD1693  [1]
 LDCM0022  KB02 HEK-293T C312(0.96)  LDD1492  [1]
 LDCM0023  KB03 HEK-293T C312(1.01)  LDD1497  [1]
 LDCM0024  KB05 HEK-293T C312(0.89)  LDD1502  [1]

References

1 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