Details of the Target

General Information of Target

Target ID LDTP04020
Target Name Cell surface glycoprotein MUC18 (MCAM)
Gene Name MCAM
Gene ID 4162
Synonyms
MUC18; Cell surface glycoprotein MUC18; Cell surface glycoprotein P1H12; Melanoma cell adhesion molecule; Melanoma-associated antigen A32; Melanoma-associated antigen MUC18; S-endo 1 endothelial-associated antigen; CD antigen CD146
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGLPRLVCAFLLAACCCCPRVAGVPGEAEQPAPELVEVEVGSTALLKCGLSQSQGNLSHV
DWFSVHKEKRTLIFRVRQGQGQSEPGEYEQRLSLQDRGATLALTQVTPQDERIFLCQGKR
PRSQEYRIQLRVYKAPEEPNIQVNPLGIPVNSKEPEEVATCVGRNGYPIPQVIWYKNGRP
LKEEKNRVHIQSSQTVESSGLYTLQSILKAQLVKEDKDAQFYCELNYRLPSGNHMKESRE
VTVPVFYPTEKVWLEVEPVGMLKEGDRVEIRCLADGNPPPHFSISKQNPSTREAEEETTN
DNGVLVLEPARKEHSGRYECQGLDLDTMISLLSEPQELLVNYVSDVRVSPAAPERQEGSS
LTLTCEAESSQDLEFQWLREETGQVLERGPVLQLHDLKREAGGGYRCVASVPSIPGLNRT
QLVNVAIFGPPWMAFKERKVWVKENMVLNLSCEASGHPRPTISWNVNGTASEQDQDPQRV
LSTLNVLVTPELLETGVECTASNDLGKNTSILFLELVNLTTLTPDSNTTTGLSTSTASPH
TRANSTSTERKLPEPESRGVVIVAVIVCILVLAVLGAVLYFLYKKGKLPCRRSGKQEITL
PPSRKSELVVEVKSDKLPEEMGLLQGSSGDKRAPGDQGEKYIDLRH
Target Type
Literature-reported
Target Bioclass
Immunoglobulin
Subcellular location
Membrane
Function
Plays a role in cell adhesion, and in cohesion of the endothelial monolayer at intercellular junctions in vascular tissue. Its expression may allow melanoma cells to interact with cellular elements of the vascular system, thereby enhancing hematogeneous tumor spread. Could be an adhesion molecule active in neural crest cells during embryonic development. Acts as a surface receptor that triggers tyrosine phosphorylation of FYN and PTK2/FAK1, and a transient increase in the intracellular calcium concentration.
TTD ID
T51569
Uniprot ID
P43121
DrugMap ID
TTHRE05
Ensemble ID
ENST00000264036.6
HGNC ID
HGNC:6934
ChEMBL ID
CHEMBL3712863

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
C32 SNV: p.S198L DBIA    Probe Info 
HCT116 SNV: p.P412S .
HCT15 SNV: p.L623I .
JURKAT Deletion: p.P431LfsTer12 .
MCC13 SNV: p.P278S DBIA    Probe Info 
MDAMB453 SNV: p.M1?; p.W377Ter DBIA    Probe Info 
MEC1 SNV: p.N151K .
MEWO SNV: p.W464Ter DBIA    Probe Info 
MFE319 SNV: p.E498G .
NCIH2286 SNV: p.V60A .
REH SNV: p.A13S .
RL952 Deletion: p.Q109KfsTer42 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		5.09  LDD0324  [1]
FBP2
 Probe Info  		2.10  LDD0323  [1]
YN-1
 Probe Info  		100.00  LDD0444  [2]
OPA-S-S-alkyne
 Probe Info  		K217(2.14); K286(2.67); K185(3.40); K182(3.40)  LDD3494  [3]
BTD
 Probe Info  		C116(0.77)  LDD2091  [4]
IPM
 Probe Info  		C116(1.69)  LDD1701  [4]
DBIA
 Probe Info  		C223(1.52)  LDD0078  [5]
5E-2FA
 Probe Info  		H281(0.00); H395(0.00); H189(0.00)  LDD2235  [6]
m-APA
 Probe Info  		H281(0.00); H189(0.00); H395(0.00)  LDD2231  [6]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [7]
PF-06672131
 Probe Info  		N.A.  LDD0152  [8]
Acrolein
 Probe Info  		H395(0.00); C116(0.00)  LDD0217  [9]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [9]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C281
 Probe Info  		5.46  LDD1951  [10]
C310
 Probe Info  		11.79  LDD1977  [10]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C116(1.27)  LDD2152  [4]
 LDCM0214  AC1 PaTu 8988t C223(0.53)  LDD1093  [5]
 LDCM0215  AC10 PaTu 8988t C223(0.85)  LDD1094  [5]
 LDCM0226  AC11 PaTu 8988t C223(0.89)  LDD1105  [5]
 LDCM0237  AC12 PaTu 8988t C223(0.86)  LDD1116  [5]
 LDCM0259  AC14 PaTu 8988t C223(1.03)  LDD1138  [5]
 LDCM0270  AC15 PaTu 8988t C223(0.92)  LDD1149  [5]
 LDCM0276  AC17 PaTu 8988t C223(1.05)  LDD1155  [5]
 LDCM0277  AC18 PaTu 8988t C223(0.56)  LDD1156  [5]
 LDCM0278  AC19 PaTu 8988t C223(0.78)  LDD1157  [5]
 LDCM0279  AC2 PaTu 8988t C223(0.67)  LDD1158  [5]
 LDCM0280  AC20 PaTu 8988t C223(0.66)  LDD1159  [5]
 LDCM0281  AC21 PaTu 8988t C223(0.43)  LDD1160  [5]
 LDCM0282  AC22 PaTu 8988t C223(0.50)  LDD1161  [5]
 LDCM0283  AC23 PaTu 8988t C223(0.46)  LDD1162  [5]
 LDCM0284  AC24 PaTu 8988t C223(1.63)  LDD1163  [5]
 LDCM0285  AC25 HEK-293T C499(0.96)  LDD1524  [11]
 LDCM0286  AC26 HEK-293T C161(1.18)  LDD1525  [11]
 LDCM0288  AC28 HEK-293T C499(0.92)  LDD1527  [11]
 LDCM0290  AC3 PaTu 8988t C223(0.58)  LDD1169  [5]
 LDCM0294  AC33 HEK-293T C499(1.04)  LDD1533  [11]
 LDCM0295  AC34 HEK-293T C161(1.00)  LDD1534  [11]
 LDCM0297  AC36 HEK-293T C499(0.87)  LDD1536  [11]
 LDCM0301  AC4 PaTu 8988t C223(0.63)  LDD1180  [5]
 LDCM0303  AC41 HEK-293T C499(1.17)  LDD1542  [11]
 LDCM0304  AC42 HEK-293T C161(1.05)  LDD1543  [11]
 LDCM0306  AC44 HEK-293T C499(0.99)  LDD1545  [11]
 LDCM0311  AC49 HEK-293T C499(0.89)  LDD1550  [11]
 LDCM0312  AC5 PaTu 8988t C223(0.54)  LDD1191  [5]
 LDCM0313  AC50 HEK-293T C161(1.29)  LDD1552  [11]
 LDCM0315  AC52 HEK-293T C499(0.96)  LDD1554  [11]
 LDCM0320  AC57 HEK-293T C499(0.98)  LDD1559  [11]
 LDCM0321  AC58 HEK-293T C161(1.02)  LDD1560  [11]
 LDCM0323  AC6 PaTu 8988t C223(1.12)  LDD1202  [5]
 LDCM0324  AC60 HEK-293T C499(1.15)  LDD1563  [11]
 LDCM0334  AC7 PaTu 8988t C223(1.06)  LDD1213  [5]
 LDCM0345  AC8 PaTu 8988t C223(0.91)  LDD1224  [5]
 LDCM0248  AKOS034007472 PaTu 8988t C223(1.18)  LDD1127  [5]
 LDCM0356  AKOS034007680 PaTu 8988t C223(0.73)  LDD1235  [5]
 LDCM0275  AKOS034007705 PaTu 8988t C223(0.91)  LDD1154  [5]
 LDCM0020  ARS-1620 HCC44 C223(1.52)  LDD0078  [5]
 LDCM0498  BS-3668 MDA-MB-231 C116(0.77)  LDD2091  [4]
 LDCM0108  Chloroacetamide HeLa C116(0.00); H395(0.00)  LDD0222  [9]
 LDCM0367  CL1 PaTu 8988t C223(1.57)  LDD1246  [5]
 LDCM0368  CL10 PaTu 8988t C223(0.96)  LDD1247  [5]
 LDCM0369  CL100 PaTu 8988t C223(0.66)  LDD1248  [5]
 LDCM0370  CL101 PaTu 8988t C223(1.06)  LDD1249  [5]
 LDCM0371  CL102 PaTu 8988t C223(0.98)  LDD1250  [5]
 LDCM0372  CL103 PaTu 8988t C223(0.94)  LDD1251  [5]
 LDCM0373  CL104 PaTu 8988t C223(1.02)  LDD1252  [5]
 LDCM0374  CL105 PaTu 8988t C223(0.66)  LDD1253  [5]
 LDCM0375  CL106 PaTu 8988t C223(1.20)  LDD1254  [5]
 LDCM0376  CL107 PaTu 8988t C223(0.96)  LDD1255  [5]
 LDCM0377  CL108 PaTu 8988t C223(0.67)  LDD1256  [5]
 LDCM0378  CL109 PaTu 8988t C223(0.63)  LDD1257  [5]
 LDCM0379  CL11 PaTu 8988t C223(1.56)  LDD1258  [5]
 LDCM0380  CL110 PaTu 8988t C223(0.70)  LDD1259  [5]
 LDCM0381  CL111 PaTu 8988t C223(0.55)  LDD1260  [5]
 LDCM0384  CL114 HEK-293T C161(1.04)  LDD1588  [11]
 LDCM0385  CL115 HEK-293T C161(0.87)  LDD1589  [11]
 LDCM0388  CL118 HEK-293T C161(0.86)  LDD1592  [11]
 LDCM0389  CL119 HEK-293T C161(0.95)  LDD1593  [11]
 LDCM0390  CL12 PaTu 8988t C223(1.15)  LDD1269  [5]
 LDCM0393  CL122 HEK-293T C161(0.88)  LDD1597  [11]
 LDCM0394  CL123 HEK-293T C161(0.87)  LDD1598  [11]
 LDCM0397  CL126 HEK-293T C161(1.12)  LDD1601  [11]
 LDCM0398  CL127 HEK-293T C161(1.06)  LDD1602  [11]
 LDCM0400  CL13 PaTu 8988t C223(0.41)  LDD1279  [5]
 LDCM0401  CL14 PaTu 8988t C223(0.33)  LDD1280  [5]
 LDCM0402  CL15 PaTu 8988t C223(1.34)  LDD1281  [5]
 LDCM0403  CL16 PaTu 8988t C223(0.78)  LDD1282  [5]
 LDCM0404  CL17 PaTu 8988t C223(0.75)  LDD1283  [5]
 LDCM0405  CL18 PaTu 8988t C223(0.74)  LDD1284  [5]
 LDCM0406  CL19 PaTu 8988t C223(0.52)  LDD1285  [5]
 LDCM0407  CL2 PaTu 8988t C223(0.71)  LDD1286  [5]
 LDCM0408  CL20 PaTu 8988t C223(0.33)  LDD1287  [5]
 LDCM0409  CL21 PaTu 8988t C223(0.29)  LDD1288  [5]
 LDCM0410  CL22 PaTu 8988t C223(0.49)  LDD1289  [5]
 LDCM0411  CL23 PaTu 8988t C223(0.60)  LDD1290  [5]
 LDCM0412  CL24 PaTu 8988t C223(1.02)  LDD1291  [5]
 LDCM0413  CL25 PaTu 8988t C223(0.94)  LDD1292  [5]
 LDCM0414  CL26 PaTu 8988t C223(0.46)  LDD1293  [5]
 LDCM0415  CL27 PaTu 8988t C223(0.71)  LDD1294  [5]
 LDCM0416  CL28 PaTu 8988t C223(0.34)  LDD1295  [5]
 LDCM0417  CL29 PaTu 8988t C223(0.38)  LDD1296  [5]
 LDCM0418  CL3 PaTu 8988t C223(1.35)  LDD1297  [5]
 LDCM0419  CL30 PaTu 8988t C223(0.93)  LDD1298  [5]
 LDCM0420  CL31 PaTu 8988t C223(0.97)  LDD1299  [5]
 LDCM0421  CL32 PaTu 8988t C223(0.95)  LDD1300  [5]
 LDCM0422  CL33 PaTu 8988t C223(1.18)  LDD1301  [5]
 LDCM0423  CL34 PaTu 8988t C223(1.05)  LDD1302  [5]
 LDCM0424  CL35 PaTu 8988t C223(1.10)  LDD1303  [5]
 LDCM0425  CL36 PaTu 8988t C223(0.37)  LDD1304  [5]
 LDCM0426  CL37 PaTu 8988t C223(1.40)  LDD1305  [5]
 LDCM0428  CL39 PaTu 8988t C223(1.10)  LDD1307  [5]
 LDCM0429  CL4 PaTu 8988t C223(1.89)  LDD1308  [5]
 LDCM0430  CL40 PaTu 8988t C223(1.09)  LDD1309  [5]
 LDCM0431  CL41 PaTu 8988t C223(1.06)  LDD1310  [5]
 LDCM0432  CL42 PaTu 8988t C223(1.19)  LDD1311  [5]
 LDCM0433  CL43 PaTu 8988t C223(1.22)  LDD1312  [5]
 LDCM0434  CL44 PaTu 8988t C223(1.30)  LDD1313  [5]
 LDCM0435  CL45 PaTu 8988t C223(1.29)  LDD1314  [5]
 LDCM0436  CL46 PaTu 8988t C223(1.11)  LDD1315  [5]
 LDCM0437  CL47 PaTu 8988t C223(1.19)  LDD1316  [5]
 LDCM0438  CL48 PaTu 8988t C223(1.09)  LDD1317  [5]
 LDCM0439  CL49 PaTu 8988t C223(1.13)  LDD1318  [5]
 LDCM0440  CL5 PaTu 8988t C223(0.40)  LDD1319  [5]
 LDCM0441  CL50 PaTu 8988t C223(1.13)  LDD1320  [5]
 LDCM0442  CL51 PaTu 8988t C223(1.42)  LDD1321  [5]
 LDCM0443  CL52 PaTu 8988t C223(1.15)  LDD1322  [5]
 LDCM0444  CL53 PaTu 8988t C223(1.24)  LDD1323  [5]
 LDCM0445  CL54 PaTu 8988t C223(1.11)  LDD1324  [5]
 LDCM0446  CL55 PaTu 8988t C223(1.15)  LDD1325  [5]
 LDCM0447  CL56 PaTu 8988t C223(0.74)  LDD1326  [5]
 LDCM0448  CL57 PaTu 8988t C223(0.73)  LDD1327  [5]
 LDCM0449  CL58 PaTu 8988t C223(0.99)  LDD1328  [5]
 LDCM0450  CL59 PaTu 8988t C223(0.79)  LDD1329  [5]
 LDCM0451  CL6 PaTu 8988t C223(0.88)  LDD1330  [5]
 LDCM0452  CL60 PaTu 8988t C223(0.88)  LDD1331  [5]
 LDCM0454  CL62 HEK-293T C161(1.08)  LDD1657  [11]
 LDCM0455  CL63 HEK-293T C161(0.93)  LDD1658  [11]
 LDCM0457  CL65 HEK-293T C499(0.96)  LDD1660  [11]
 LDCM0458  CL66 HEK-293T C161(1.04)  LDD1661  [11]
 LDCM0460  CL68 HEK-293T C499(0.95)  LDD1663  [11]
 LDCM0462  CL7 PaTu 8988t C223(0.56)  LDD1341  [5]
 LDCM0467  CL74 HEK-293T C161(0.89)  LDD1670  [11]
 LDCM0470  CL77 HEK-293T C499(0.90)  LDD1673  [11]
 LDCM0471  CL78 HEK-293T C161(1.15)  LDD1674  [11]
 LDCM0473  CL8 PaTu 8988t C223(0.99)  LDD1352  [5]
 LDCM0474  CL80 HEK-293T C499(1.01)  LDD1677  [11]
 LDCM0480  CL86 HEK-293T C161(0.89)  LDD1683  [11]
 LDCM0481  CL87 HEK-293T C161(1.05)  LDD1684  [11]
 LDCM0483  CL89 HEK-293T C499(0.86)  LDD1686  [11]
 LDCM0484  CL9 PaTu 8988t C223(0.53)  LDD1363  [5]
 LDCM0485  CL90 HEK-293T C161(1.19)  LDD1688  [11]
 LDCM0486  CL91 PaTu 8988t C223(0.56)  LDD1365  [5]
 LDCM0487  CL92 PaTu 8988t C223(0.61)  LDD1366  [5]
 LDCM0488  CL93 PaTu 8988t C223(0.65)  LDD1367  [5]
 LDCM0489  CL94 PaTu 8988t C223(0.63)  LDD1368  [5]
 LDCM0490  CL95 PaTu 8988t C223(0.53)  LDD1369  [5]
 LDCM0491  CL96 PaTu 8988t C223(0.63)  LDD1370  [5]
 LDCM0492  CL97 PaTu 8988t C223(0.61)  LDD1371  [5]
 LDCM0493  CL98 PaTu 8988t C223(0.77)  LDD1372  [5]
 LDCM0494  CL99 PaTu 8988t C223(0.66)  LDD1373  [5]
 LDCM0495  E2913 HEK-293T C161(1.06)  LDD1698  [11]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C116(0.78)  LDD1702  [4]
 LDCM0468  Fragment33 HEK-293T C161(1.04)  LDD1671  [11]
 LDCM0427  Fragment51 PaTu 8988t C223(1.27)  LDD1306  [5]
 LDCM0107  IAA HeLa N.A.  LDD0221  [9]
 LDCM0022  KB02 HEK-293T C161(1.00)  LDD1492  [11]
 LDCM0023  KB03 HEK-293T C161(1.01)  LDD1497  [11]
 LDCM0024  KB05 COLO792 C223(1.58)  LDD3310  [12]
 LDCM0109  NEM HeLa N.A.  LDD0225  [9]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C116(1.17)  LDD2093  [4]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C116(1.07)  LDD2097  [4]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C116(0.96)  LDD2099  [4]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C116(0.85)  LDD2107  [4]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C116(1.07)  LDD2129  [4]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C116(0.95)  LDD2133  [4]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C116(0.84)  LDD2134  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C116(0.86)  LDD2136  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C116(0.63)  LDD2140  [4]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C116(1.03)  LDD2143  [4]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C116(2.65)  LDD2144  [4]

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
2 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.
3 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
4 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
5 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.
6 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
7 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
8 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
9 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
10 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
11 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
12 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