Details of the Target

General Information of Target

Target ID LDTP01262
Target Name Low-density lipoprotein receptor-related protein 6 (LRP6)
Gene Name LRP6
Gene ID 4040
Synonyms
Low-density lipoprotein receptor-related protein 6; LRP-6
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGAVLRSLLACSFCVLLRAAPLLLYANRRDLRLVDATNGKENATIVVGGLEDAAAVDFVF
SHGLIYWSDVSEEAIKRTEFNKTESVQNVVVSGLLSPDGLACDWLGEKLYWTDSETNRIE
VSNLDGSLRKVLFWQELDQPRAIALDPSSGFMYWTDWGEVPKIERAGMDGSSRFIIINSE
IYWPNGLTLDYEEQKLYWADAKLNFIHKSNLDGTNRQAVVKGSLPHPFALTLFEDILYWT
DWSTHSILACNKYTGEGLREIHSDIFSPMDIHAFSQQRQPNATNPCGIDNGGCSHLCLMS
PVKPFYQCACPTGVKLLENGKTCKDGATELLLLARRTDLRRISLDTPDFTDIVLQLEDIR
HAIAIDYDPVEGYIYWTDDEVRAIRRSFIDGSGSQFVVTAQIAHPDGIAVDWVARNLYWT
DTGTDRIEVTRLNGTMRKILISEDLEEPRAIVLDPMVGYMYWTDWGEIPKIERAALDGSD
RVVLVNTSLGWPNGLALDYDEGKIYWGDAKTDKIEVMNTDGTGRRVLVEDKIPHIFGFTL
LGDYVYWTDWQRRSIERVHKRSAEREVIIDQLPDLMGLKATNVHRVIGSNPCAEENGGCS
HLCLYRPQGLRCACPIGFELISDMKTCIVPEAFLLFSRRADIRRISLETNNNNVAIPLTG
VKEASALDFDVTDNRIYWTDISLKTISRAFMNGSALEHVVEFGLDYPEGMAVDWLGKNLY
WADTGTNRIEVSKLDGQHRQVLVWKDLDSPRALALDPAEGFMYWTEWGGKPKIDRAAMDG
SERTTLVPNVGRANGLTIDYAKRRLYWTDLDTNLIESSNMLGLNREVIADDLPHPFGLTQ
YQDYIYWTDWSRRSIERANKTSGQNRTIIQGHLDYVMDILVFHSSRQSGWNECASSNGHC
SHLCLAVPVGGFVCGCPAHYSLNADNRTCSAPTTFLLFSQKSAINRMVIDEQQSPDIILP
IHSLRNVRAIDYDPLDKQLYWIDSRQNMIRKAQEDGSQGFTVVVSSVPSQNLEIQPYDLS
IDIYSRYIYWTCEATNVINVTRLDGRSVGVVLKGEQDRPRAVVVNPEKGYMYFTNLQERS
PKIERAALDGTEREVLFFSGLSKPIALALDSRLGKLFWADSDLRRIESSDLSGANRIVLE
DSNILQPVGLTVFENWLYWIDKQQQMIEKIDMTGREGRTKVQARIAQLSDIHAVKELNLQ
EYRQHPCAQDNGGCSHICLVKGDGTTRCSCPMHLVLLQDELSCGEPPTCSPQQFTCFTGE
IDCIPVAWRCDGFTECEDHSDELNCPVCSESQFQCASGQCIDGALRCNGDANCQDKSDEK
NCEVLCLIDQFRCANGQCIGKHKKCDHNVDCSDKSDELDCYPTEEPAPQATNTVGSVIGV
IVTIFVSGTVYFICQRMLCPRMKGDGETMTNDYVVHGPASVPLGYVPHPSSLSGSLPGMS
RGKSMISSLSIMGGSSGPPYDRAHVTGASSSSSSSTKGTYFPAILNPPPSPATERSHYTM
EFGYSSNSPSTHRSYSYRPYSYRHFAPPTTPCSTDVCDSDYAPSRRMTSVATAKGYTSDL
NYDSEPVPPPPTPRSQYLSAEENYESCPPSPYTERSYSHHLYPPPPSPCTDSS
Target Type
Clinical trial
Target Bioclass
Other
Family
LDLR family
Subcellular location
Cell membrane
Function
Component of the Wnt-Fzd-LRP5-LRP6 complex that triggers beta-catenin signaling through inducing aggregation of receptor-ligand complexes into ribosome-sized signalosomes. Cell-surface coreceptor of Wnt/beta-catenin signaling, which plays a pivotal role in bone formation. The Wnt-induced Fzd/LRP6 coreceptor complex recruits DVL1 polymers to the plasma membrane which, in turn, recruits the AXIN1/GSK3B-complex to the cell surface promoting the formation of signalosomes and inhibiting AXIN1/GSK3-mediated phosphorylation and destruction of beta-catenin. Required for posterior patterning of the epiblast during gastrulation.
TTD ID
T49755
Uniprot ID
O75581
DrugMap ID
TTSXOWE
Ensemble ID
ENST00000261349.9
HGNC ID
HGNC:6698
ChEMBL ID
CHEMBL3745588

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
OPA-S-S-alkyne
 Probe Info  		K1053(2.76)  LDD3494  [1]
DBIA
 Probe Info  		C1532(1.01); C1537(1.01); C1333(0.94); C1338(0.94)  LDD0078  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C102(0.94); C612(1.65)  LDD1507  [3]
 LDCM0226  AC11 HEK-293T C612(1.29)  LDD1509  [3]
 LDCM0259  AC14 HEK-293T C929(1.09); C1333(1.07); C612(1.11)  LDD1512  [3]
 LDCM0270  AC15 HEK-293T C1333(0.97)  LDD1513  [3]
 LDCM0276  AC17 HEK-293T C102(0.92); C612(0.99)  LDD1515  [3]
 LDCM0278  AC19 HEK-293T C612(1.08)  LDD1517  [3]
 LDCM0281  AC21 HEK-293T C1587(0.85); C1333(0.91); C1322(0.89)  LDD1520  [3]
 LDCM0282  AC22 HEK-293T C929(0.98); C1333(1.05); C612(1.00)  LDD1521  [3]
 LDCM0283  AC23 HEK-293T C1333(0.93)  LDD1522  [3]
 LDCM0284  AC24 HEK-293T C1587(0.96); C102(0.95)  LDD1523  [3]
 LDCM0285  AC25 HEK-293T C102(0.90); C612(1.22)  LDD1524  [3]
 LDCM0287  AC27 HEK-293T C612(1.04)  LDD1526  [3]
 LDCM0289  AC29 HEK-293T C1587(0.83); C1333(0.95); C1322(0.91)  LDD1528  [3]
 LDCM0290  AC3 HEK-293T C612(1.29)  LDD1529  [3]
 LDCM0291  AC30 HEK-293T C929(1.02); C1333(0.93); C612(0.88)  LDD1530  [3]
 LDCM0292  AC31 HEK-293T C1333(0.93)  LDD1531  [3]
 LDCM0293  AC32 HEK-293T C1587(0.78); C102(0.91)  LDD1532  [3]
 LDCM0294  AC33 HEK-293T C102(1.12); C612(1.52)  LDD1533  [3]
 LDCM0296  AC35 HEK-293T C612(1.19)  LDD1535  [3]
 LDCM0298  AC37 HEK-293T C1587(1.06); C1333(0.88); C1322(1.00)  LDD1537  [3]
 LDCM0299  AC38 HEK-293T C929(1.10); C1333(0.97); C612(1.11)  LDD1538  [3]
 LDCM0300  AC39 HEK-293T C1333(1.04)  LDD1539  [3]
 LDCM0302  AC40 HEK-293T C1587(1.00); C102(1.10)  LDD1541  [3]
 LDCM0303  AC41 HEK-293T C102(1.04); C612(1.12)  LDD1542  [3]
 LDCM0305  AC43 HEK-293T C612(1.12)  LDD1544  [3]
 LDCM0307  AC45 HEK-293T C1587(1.15); C1333(0.98); C1322(0.97)  LDD1546  [3]
 LDCM0308  AC46 HEK-293T C929(1.12); C1333(1.02); C612(1.24)  LDD1547  [3]
 LDCM0309  AC47 HEK-293T C1333(0.98)  LDD1548  [3]
 LDCM0310  AC48 HEK-293T C1587(1.00); C102(0.99)  LDD1549  [3]
 LDCM0311  AC49 HEK-293T C102(1.05); C612(1.39)  LDD1550  [3]
 LDCM0312  AC5 HEK-293T C1587(0.93); C1333(0.93); C1322(1.02)  LDD1551  [3]
 LDCM0314  AC51 HEK-293T C612(1.27)  LDD1553  [3]
 LDCM0316  AC53 HEK-293T C1587(1.04); C1333(0.90); C1322(1.03)  LDD1555  [3]
 LDCM0317  AC54 HEK-293T C929(1.05); C1333(1.13); C612(0.81)  LDD1556  [3]
 LDCM0318  AC55 HEK-293T C1333(1.02)  LDD1557  [3]
 LDCM0319  AC56 HEK-293T C1587(1.30); C102(0.99)  LDD1558  [3]
 LDCM0320  AC57 HEK-293T C102(0.97); C612(1.34)  LDD1559  [3]
 LDCM0322  AC59 HEK-293T C612(1.29)  LDD1561  [3]
 LDCM0323  AC6 HEK-293T C929(0.90); C1333(1.09); C612(0.91)  LDD1562  [3]
 LDCM0325  AC61 HEK-293T C1587(0.92); C1333(0.97); C1322(1.09)  LDD1564  [3]
 LDCM0326  AC62 HEK-293T C929(1.17); C1333(0.97); C612(0.96)  LDD1565  [3]
 LDCM0327  AC63 HEK-293T C1333(0.98)  LDD1566  [3]
 LDCM0328  AC64 HEK-293T C1587(1.08); C102(1.09)  LDD1567  [3]
 LDCM0334  AC7 HEK-293T C1333(0.98)  LDD1568  [3]
 LDCM0345  AC8 HEK-293T C1587(0.97); C102(0.99)  LDD1569  [3]
 LDCM0248  AKOS034007472 HEK-293T C1587(0.82); C1333(0.97); C1322(1.02)  LDD1511  [3]
 LDCM0356  AKOS034007680 HEK-293T C102(1.08); C612(1.26)  LDD1570  [3]
 LDCM0275  AKOS034007705 HEK-293T C1587(1.01); C102(1.07)  LDD1514  [3]
 LDCM0020  ARS-1620 HCC44 C1532(1.01); C1537(1.01); C1333(0.94); C1338(0.94)  LDD0078  [2]
 LDCM0367  CL1 HEK-293T C614(1.03)  LDD1571  [3]
 LDCM0368  CL10 HEK-293T C929(1.38); C1333(1.09); C612(1.02)  LDD1572  [3]
 LDCM0369  CL100 HEK-293T C1587(0.87)  LDD1573  [3]
 LDCM0370  CL101 HEK-293T C614(0.77)  LDD1574  [3]
 LDCM0372  CL103 HEK-293T C102(1.07); C929(0.85); C1326(1.18); C614(1.09)  LDD1576  [3]
 LDCM0373  CL104 HEK-293T C1587(1.01)  LDD1577  [3]
 LDCM0374  CL105 HEK-293T C614(0.91)  LDD1578  [3]
 LDCM0376  CL107 HEK-293T C102(0.83); C929(1.10); C1326(0.94); C614(0.92)  LDD1580  [3]
 LDCM0377  CL108 HEK-293T C1587(0.99)  LDD1581  [3]
 LDCM0378  CL109 HEK-293T C614(1.08)  LDD1582  [3]
 LDCM0379  CL11 HEK-293T C1333(0.88)  LDD1583  [3]
 LDCM0381  CL111 HEK-293T C102(0.94); C929(1.15); C1326(0.95); C614(0.68)  LDD1585  [3]
 LDCM0382  CL112 HEK-293T C1587(0.81)  LDD1586  [3]
 LDCM0383  CL113 HEK-293T C614(0.74)  LDD1587  [3]
 LDCM0385  CL115 HEK-293T C102(0.86); C929(1.00); C1326(0.90); C614(1.17)  LDD1589  [3]
 LDCM0386  CL116 HEK-293T C1587(0.79)  LDD1590  [3]
 LDCM0387  CL117 HEK-293T C614(0.85)  LDD1591  [3]
 LDCM0389  CL119 HEK-293T C102(0.92); C929(1.08); C1326(0.97); C614(1.23)  LDD1593  [3]
 LDCM0390  CL12 HEK-293T C1587(1.43); C102(1.27)  LDD1594  [3]
 LDCM0391  CL120 HEK-293T C1587(0.76)  LDD1595  [3]
 LDCM0392  CL121 HEK-293T C614(0.89)  LDD1596  [3]
 LDCM0394  CL123 HEK-293T C102(0.35); C929(1.04); C1326(1.14); C614(1.16)  LDD1598  [3]
 LDCM0395  CL124 HEK-293T C1587(1.03)  LDD1599  [3]
 LDCM0396  CL125 HEK-293T C614(0.69)  LDD1600  [3]
 LDCM0398  CL127 HEK-293T C102(0.97); C929(0.97); C1326(0.97); C614(1.06)  LDD1602  [3]
 LDCM0399  CL128 HEK-293T C1587(0.76)  LDD1603  [3]
 LDCM0400  CL13 HEK-293T C614(0.91)  LDD1604  [3]
 LDCM0402  CL15 HEK-293T C102(0.94); C929(0.85); C1326(1.07); C614(0.88)  LDD1606  [3]
 LDCM0403  CL16 HEK-293T C1587(1.10)  LDD1607  [3]
 LDCM0404  CL17 HEK-293T C102(0.99); C612(1.44)  LDD1608  [3]
 LDCM0406  CL19 HEK-293T C612(1.29)  LDD1610  [3]
 LDCM0409  CL21 HEK-293T C1587(1.00); C1333(0.93); C1322(1.01)  LDD1613  [3]
 LDCM0410  CL22 HEK-293T C929(1.02); C1333(1.04); C612(1.28)  LDD1614  [3]
 LDCM0411  CL23 HEK-293T C1333(1.00)  LDD1615  [3]
 LDCM0412  CL24 HEK-293T C1587(0.70); C102(1.13)  LDD1616  [3]
 LDCM0413  CL25 HEK-293T C614(0.60)  LDD1617  [3]
 LDCM0415  CL27 HEK-293T C102(0.99); C929(1.07); C1326(0.94); C614(0.93)  LDD1619  [3]
 LDCM0416  CL28 HEK-293T C1587(0.75)  LDD1620  [3]
 LDCM0417  CL29 HEK-293T C102(0.99); C612(1.13)  LDD1621  [3]
 LDCM0418  CL3 HEK-293T C102(1.18); C929(1.02); C1326(1.18); C614(0.81)  LDD1622  [3]
 LDCM0420  CL31 HEK-293T C612(1.28)  LDD1624  [3]
 LDCM0422  CL33 HEK-293T C1587(1.57); C1333(0.96); C1322(1.51)  LDD1626  [3]
 LDCM0423  CL34 HEK-293T C929(0.92); C1333(1.12); C612(1.15)  LDD1627  [3]
 LDCM0424  CL35 HEK-293T C1333(1.02)  LDD1628  [3]
 LDCM0425  CL36 HEK-293T C1587(0.73); C102(1.14)  LDD1629  [3]
 LDCM0426  CL37 HEK-293T C614(1.19)  LDD1630  [3]
 LDCM0428  CL39 HEK-293T C102(1.01); C929(1.07); C1326(0.93); C614(0.87)  LDD1632  [3]
 LDCM0429  CL4 HEK-293T C1587(0.88)  LDD1633  [3]
 LDCM0430  CL40 HEK-293T C1587(0.89)  LDD1634  [3]
 LDCM0431  CL41 HEK-293T C102(1.04); C612(1.11)  LDD1635  [3]
 LDCM0433  CL43 HEK-293T C612(1.23)  LDD1637  [3]
 LDCM0435  CL45 HEK-293T C1587(0.68); C1333(1.02); C1322(2.15)  LDD1639  [3]
 LDCM0436  CL46 HEK-293T C929(0.95); C1333(1.00); C612(1.04)  LDD1640  [3]
 LDCM0437  CL47 HEK-293T C1333(1.03)  LDD1641  [3]
 LDCM0438  CL48 HEK-293T C1587(0.99); C102(1.33)  LDD1642  [3]
 LDCM0439  CL49 HEK-293T C614(0.75)  LDD1643  [3]
 LDCM0440  CL5 HEK-293T C102(0.99); C612(1.21)  LDD1644  [3]
 LDCM0443  CL52 HEK-293T C1587(0.99)  LDD1646  [3]
 LDCM0444  CL53 HEK-293T C102(1.09); C612(1.08)  LDD1647  [3]
 LDCM0446  CL55 HEK-293T C612(1.30)  LDD1649  [3]
 LDCM0448  CL57 HEK-293T C1587(0.94); C1333(0.89); C1322(1.89)  LDD1651  [3]
 LDCM0449  CL58 HEK-293T C929(1.00); C1333(1.19); C612(0.98)  LDD1652  [3]
 LDCM0450  CL59 HEK-293T C1333(0.95)  LDD1653  [3]
 LDCM0452  CL60 HEK-293T C1587(1.57); C102(1.32)  LDD1655  [3]
 LDCM0453  CL61 HEK-293T C614(0.71)  LDD1656  [3]
 LDCM0455  CL63 HEK-293T C102(0.97); C929(1.01); C1326(0.92); C614(1.67)  LDD1658  [3]
 LDCM0456  CL64 HEK-293T C1587(0.80)  LDD1659  [3]
 LDCM0457  CL65 HEK-293T C102(1.01); C612(1.18)  LDD1660  [3]
 LDCM0459  CL67 HEK-293T C612(1.35)  LDD1662  [3]
 LDCM0461  CL69 HEK-293T C1587(0.91); C1333(0.97); C1322(0.99)  LDD1664  [3]
 LDCM0462  CL7 HEK-293T C612(1.50)  LDD1665  [3]
 LDCM0463  CL70 HEK-293T C929(0.87); C1333(1.12); C612(0.99)  LDD1666  [3]
 LDCM0464  CL71 HEK-293T C1333(1.04)  LDD1667  [3]
 LDCM0465  CL72 HEK-293T C1587(1.23); C102(1.13)  LDD1668  [3]
 LDCM0466  CL73 HEK-293T C614(0.69)  LDD1669  [3]
 LDCM0469  CL76 HEK-293T C1587(0.91)  LDD1672  [3]
 LDCM0470  CL77 HEK-293T C102(1.00); C612(1.10)  LDD1673  [3]
 LDCM0472  CL79 HEK-293T C612(1.29)  LDD1675  [3]
 LDCM0475  CL81 HEK-293T C1587(1.21); C1333(0.98); C1322(0.99)  LDD1678  [3]
 LDCM0476  CL82 HEK-293T C929(1.03); C1333(1.01); C612(0.91)  LDD1679  [3]
 LDCM0477  CL83 HEK-293T C1333(1.04)  LDD1680  [3]
 LDCM0478  CL84 HEK-293T C1587(0.61); C102(0.76)  LDD1681  [3]
 LDCM0479  CL85 HEK-293T C614(0.80)  LDD1682  [3]
 LDCM0481  CL87 HEK-293T C102(0.85); C929(1.03); C1326(0.91); C614(0.85)  LDD1684  [3]
 LDCM0482  CL88 HEK-293T C1587(0.98)  LDD1685  [3]
 LDCM0483  CL89 HEK-293T C102(1.03); C612(1.37)  LDD1686  [3]
 LDCM0484  CL9 HEK-293T C1587(0.82); C1333(0.85); C1322(1.03)  LDD1687  [3]
 LDCM0486  CL91 HEK-293T C612(1.12)  LDD1689  [3]
 LDCM0488  CL93 HEK-293T C1587(0.91); C1333(1.00); C1322(1.12)  LDD1691  [3]
 LDCM0489  CL94 HEK-293T C929(1.13); C1333(0.93); C612(1.17)  LDD1692  [3]
 LDCM0490  CL95 HEK-293T C1333(0.92)  LDD1693  [3]
 LDCM0491  CL96 HEK-293T C1587(1.02); C102(0.77)  LDD1694  [3]
 LDCM0492  CL97 HEK-293T C614(0.72)  LDD1695  [3]
 LDCM0494  CL99 HEK-293T C102(0.91); C929(1.00); C1326(1.10); C614(1.12)  LDD1697  [3]
 LDCM0495  E2913 HEK-293T C102(0.91); C929(0.93); C1326(0.97); C614(0.98)  LDD1698  [3]
 LDCM0468  Fragment33 HEK-293T C102(0.97); C929(1.21); C1326(1.03); C614(1.21)  LDD1671  [3]
 LDCM0021  THZ1 HCT 116 C1532(1.10); C1537(1.10)  LDD2173  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Glycogen synthase kinase-3 alpha (GSK3A) CMGC Ser/Thr protein kinase family P49840
Glycogen synthase kinase-3 beta (GSK3B) CMGC Ser/Thr protein kinase family P49841
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) TKL Ser/Thr protein kinase family Q5S007
Platelet-derived growth factor receptor beta (PDGFRB) Tyr protein kinase family P09619
E3 ubiquitin-protein ligase ZNRF3 (ZNRF3) ZNRF3 family Q9ULT6
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Caveolin-1 (CAV1) Caveolin family Q03135
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Chemokine-like factor (CKLF) Chemokine-like factor family Q9UBR5
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Anthrax toxin receptor 1 (ANTXR1) ATR family Q9H6X2
Dickkopf-related protein 1 (DKK1) Dickkopf family O94907
Low-density lipoprotein receptor-related protein 6 (LRP6) LDLR family O75581
Sclerostin (SOST) Sclerostin family Q9BQB4
Protein Wnt-3a (WNT3A) Wnt family P56704
Disabled homolog 2 (DAB2) . P98082
Nuclear protein AMMECR1 (AMMECR1) . Q9Y4X0

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bi 905677 Antibody DTB43H

References

1 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
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 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