General Information of Target

Target ID LDTP11366
Target Name Leucine-rich repeat-containing G-protein coupled receptor 4 (LGR4)
Gene Name LGR4
Gene ID 55366
Synonyms
GPR48; Leucine-rich repeat-containing G-protein coupled receptor 4; G-protein coupled receptor 48
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDDAAVLKRRGYLLGINLGEGSYAKVKSAYSERLKFNVAIKIIDRKKAPADFLEKFLPRE
IEILAMLNHCSIIKTYEIFETSHGKVYIVMELAVQGDLLELIKTRGALHEDEARKKFHQL
SLAIKYCHDLDVVHRDLKCDNLLLDKDFNIKLSDFSFSKRCLRDDSGRMALSKTFCGSPA
YAAPEVLQGIPYQPKVYDIWSLGVILYIMVCGSMPYDDSNIKKMLRIQKEHRVNFPRSKH
LTGECKDLIYHMLQPDVNRRLHIDEILSHCWMQPKARGSPSVAINKEGESSRGTEPLWTP
EPGSDKKSATKLEPEGEAQPQAQPETKPEGTAMQMSRQSEILGFPSKPSTMETEEGPPQQ
PPETRAQ
Target Type
Preclinical
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell membrane
Function
Receptor for R-spondins that potentiates the canonical Wnt signaling pathway and is involved in the formation of various organs. Upon binding to R-spondins (RSPO1, RSPO2, RSPO3 or RSPO4), associates with phosphorylated LRP6 and frizzled receptors that are activated by extracellular Wnt receptors, triggering the canonical Wnt signaling pathway to increase expression of target genes. In contrast to classical G-protein coupled receptors, does not activate heterotrimeric G-proteins to transduce the signal. Its function as activator of the Wnt signaling pathway is required for the development of various organs, including liver, kidney, intestine, bone, reproductive tract and eye. May also act as a receptor for norrin (NDP), such results however require additional confirmation in vivo. Required during spermatogenesis to activate the Wnt signaling pathway in peritubular myoid cells. Required for the maintenance of intestinal stem cells and Paneth cell differentiation in postnatal intestinal crypts. Acts as a regulator of bone formation and remodeling. Involved in kidney development; required for maintaining the ureteric bud in an undifferentiated state. Involved in the development of the anterior segment of the eye. Required during erythropoiesis. Also acts as a negative regulator of innate immunity by inhibiting TLR2/TLR4 associated pattern-recognition and pro-inflammatory cytokine production. Plays an important role in regulating the circadian rhythms of plasma lipids, partially through regulating the rhythmic expression of MTTP. Required for proper development of GnRH neurons (gonadotropin-releasing hormone expressing neurons) that control the release of reproductive hormones from the pituitary gland.
TTD ID
T90672
Uniprot ID
Q9BXB1
DrugMap ID
TTY6C71
Ensemble ID
ENST00000379214.9
HGNC ID
HGNC:13299

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.L203R .
JURKAT SNV: p.G603S .
KMRC1 SNV: p.R663G .
MOLT4 SNV: p.Y687F; p.S784F .
NCIH2286 SNV: p.V545L .

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 
C930(1.78)  LDD3367  [1]
IPM
 Probe Info 
N.A.  LDD0147  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C930(1.04)  LDD1507  [3]
 LDCM0215  AC10 HEK-293T C930(1.09)  LDD1508  [3]
 LDCM0237  AC12 HEK-293T C339(1.02); C930(0.94)  LDD1510  [3]
 LDCM0259  AC14 HEK-293T C930(0.97)  LDD1512  [3]
 LDCM0270  AC15 HEK-293T C930(1.06)  LDD1513  [3]
 LDCM0276  AC17 HEK-293T C930(1.05)  LDD1515  [3]
 LDCM0277  AC18 HEK-293T C930(1.04)  LDD1516  [3]
 LDCM0279  AC2 HEK-293T C930(1.08)  LDD1518  [3]
 LDCM0280  AC20 HEK-293T C339(1.04); C930(0.95)  LDD1519  [3]
 LDCM0281  AC21 HEK-293T C930(0.92)  LDD1520  [3]
 LDCM0282  AC22 HEK-293T C930(0.89)  LDD1521  [3]
 LDCM0283  AC23 HEK-293T C930(0.96)  LDD1522  [3]
 LDCM0284  AC24 HEK-293T C930(0.98)  LDD1523  [3]
 LDCM0285  AC25 HEK-293T C930(1.08)  LDD1524  [3]
 LDCM0286  AC26 HEK-293T C930(1.10)  LDD1525  [3]
 LDCM0288  AC28 HEK-293T C339(1.04); C930(1.01)  LDD1527  [3]
 LDCM0289  AC29 HEK-293T C930(0.92)  LDD1528  [3]
 LDCM0291  AC30 HEK-293T C930(1.00)  LDD1530  [3]
 LDCM0292  AC31 HEK-293T C930(0.97)  LDD1531  [3]
 LDCM0293  AC32 HEK-293T C930(0.98)  LDD1532  [3]
 LDCM0294  AC33 HEK-293T C930(1.02)  LDD1533  [3]
 LDCM0295  AC34 HEK-293T C930(1.06)  LDD1534  [3]
 LDCM0297  AC36 HEK-293T C339(1.10); C930(0.94)  LDD1536  [3]
 LDCM0298  AC37 HEK-293T C930(0.96)  LDD1537  [3]
 LDCM0299  AC38 HEK-293T C930(0.92)  LDD1538  [3]
 LDCM0300  AC39 HEK-293T C930(1.01)  LDD1539  [3]
 LDCM0301  AC4 HEK-293T C339(1.04); C930(1.02)  LDD1540  [3]
 LDCM0302  AC40 HEK-293T C930(0.96)  LDD1541  [3]
 LDCM0303  AC41 HEK-293T C930(1.09)  LDD1542  [3]
 LDCM0304  AC42 HEK-293T C930(1.14)  LDD1543  [3]
 LDCM0306  AC44 HEK-293T C339(1.03); C930(1.01)  LDD1545  [3]
 LDCM0307  AC45 HEK-293T C930(0.97)  LDD1546  [3]
 LDCM0308  AC46 HEK-293T C930(1.04)  LDD1547  [3]
 LDCM0309  AC47 HEK-293T C930(0.99)  LDD1548  [3]
 LDCM0310  AC48 HEK-293T C930(0.98)  LDD1549  [3]
 LDCM0311  AC49 HEK-293T C930(0.94)  LDD1550  [3]
 LDCM0312  AC5 HEK-293T C930(1.16)  LDD1551  [3]
 LDCM0313  AC50 HEK-293T C930(1.07)  LDD1552  [3]
 LDCM0315  AC52 HEK-293T C339(1.04); C930(1.00)  LDD1554  [3]
 LDCM0316  AC53 HEK-293T C930(1.00)  LDD1555  [3]
 LDCM0317  AC54 HEK-293T C930(1.08)  LDD1556  [3]
 LDCM0318  AC55 HEK-293T C930(0.97)  LDD1557  [3]
 LDCM0319  AC56 HEK-293T C930(0.93)  LDD1558  [3]
 LDCM0320  AC57 HEK-293T C930(1.03)  LDD1559  [3]
 LDCM0321  AC58 HEK-293T C930(1.04)  LDD1560  [3]
 LDCM0323  AC6 HEK-293T C930(1.01)  LDD1562  [3]
 LDCM0324  AC60 HEK-293T C339(1.05); C930(0.96)  LDD1563  [3]
 LDCM0325  AC61 HEK-293T C930(1.03)  LDD1564  [3]
 LDCM0326  AC62 HEK-293T C930(1.00)  LDD1565  [3]
 LDCM0327  AC63 HEK-293T C930(1.06)  LDD1566  [3]
 LDCM0328  AC64 HEK-293T C930(1.00)  LDD1567  [3]
 LDCM0334  AC7 HEK-293T C930(1.04)  LDD1568  [3]
 LDCM0345  AC8 HEK-293T C930(0.92)  LDD1569  [3]
 LDCM0248  AKOS034007472 HEK-293T C930(1.03)  LDD1511  [3]
 LDCM0356  AKOS034007680 HEK-293T C930(1.14)  LDD1570  [3]
 LDCM0275  AKOS034007705 HEK-293T C930(1.00)  LDD1514  [3]
 LDCM0367  CL1 HEK-293T C930(1.11)  LDD1571  [3]
 LDCM0368  CL10 HEK-293T C930(1.17)  LDD1572  [3]
 LDCM0369  CL100 HEK-293T C930(1.02)  LDD1573  [3]
 LDCM0370  CL101 HEK-293T C930(0.98)  LDD1574  [3]
 LDCM0371  CL102 HEK-293T C930(1.25)  LDD1575  [3]
 LDCM0372  CL103 HEK-293T C930(1.03)  LDD1576  [3]
 LDCM0373  CL104 HEK-293T C930(0.99)  LDD1577  [3]
 LDCM0374  CL105 HEK-293T C930(0.91)  LDD1578  [3]
 LDCM0375  CL106 HEK-293T C930(1.01)  LDD1579  [3]
 LDCM0376  CL107 HEK-293T C930(0.90)  LDD1580  [3]
 LDCM0377  CL108 HEK-293T C930(1.07)  LDD1581  [3]
 LDCM0378  CL109 HEK-293T C930(1.07)  LDD1582  [3]
 LDCM0379  CL11 HEK-293T C930(1.05)  LDD1583  [3]
 LDCM0380  CL110 HEK-293T C930(1.20)  LDD1584  [3]
 LDCM0381  CL111 HEK-293T C930(0.94)  LDD1585  [3]
 LDCM0382  CL112 HEK-293T C930(0.98)  LDD1586  [3]
 LDCM0383  CL113 HEK-293T C930(1.03)  LDD1587  [3]
 LDCM0384  CL114 HEK-293T C930(1.19)  LDD1588  [3]
 LDCM0385  CL115 HEK-293T C930(0.84)  LDD1589  [3]
 LDCM0386  CL116 HEK-293T C930(1.17)  LDD1590  [3]
 LDCM0387  CL117 HEK-293T C930(1.07)  LDD1591  [3]
 LDCM0388  CL118 HEK-293T C930(1.15)  LDD1592  [3]
 LDCM0389  CL119 HEK-293T C930(0.98)  LDD1593  [3]
 LDCM0390  CL12 HEK-293T C930(1.14)  LDD1594  [3]
 LDCM0391  CL120 HEK-293T C930(1.04)  LDD1595  [3]
 LDCM0392  CL121 HEK-293T C930(1.01)  LDD1596  [3]
 LDCM0393  CL122 HEK-293T C930(1.15)  LDD1597  [3]
 LDCM0394  CL123 HEK-293T C930(1.12)  LDD1598  [3]
 LDCM0395  CL124 HEK-293T C930(1.06)  LDD1599  [3]
 LDCM0396  CL125 HEK-293T C930(1.09)  LDD1600  [3]
 LDCM0397  CL126 HEK-293T C930(1.05)  LDD1601  [3]
 LDCM0398  CL127 HEK-293T C930(1.02)  LDD1602  [3]
 LDCM0399  CL128 HEK-293T C930(1.03)  LDD1603  [3]
 LDCM0400  CL13 HEK-293T C930(1.02)  LDD1604  [3]
 LDCM0401  CL14 HEK-293T C930(1.08)  LDD1605  [3]
 LDCM0402  CL15 HEK-293T C930(1.03)  LDD1606  [3]
 LDCM0403  CL16 HEK-293T C930(1.10)  LDD1607  [3]
 LDCM0404  CL17 HEK-293T C930(1.14)  LDD1608  [3]
 LDCM0405  CL18 HEK-293T C930(1.03)  LDD1609  [3]
 LDCM0407  CL2 HEK-293T C930(1.02)  LDD1611  [3]
 LDCM0408  CL20 HEK-293T C339(1.17); C930(0.95)  LDD1612  [3]
 LDCM0409  CL21 HEK-293T C930(1.14)  LDD1613  [3]
 LDCM0410  CL22 HEK-293T C930(1.07)  LDD1614  [3]
 LDCM0411  CL23 HEK-293T C930(1.01)  LDD1615  [3]
 LDCM0412  CL24 HEK-293T C930(1.16)  LDD1616  [3]
 LDCM0413  CL25 HEK-293T C930(1.04)  LDD1617  [3]
 LDCM0414  CL26 HEK-293T C930(1.19)  LDD1618  [3]
 LDCM0415  CL27 HEK-293T C930(0.85)  LDD1619  [3]
 LDCM0416  CL28 HEK-293T C930(1.05)  LDD1620  [3]
 LDCM0417  CL29 HEK-293T C930(1.17)  LDD1621  [3]
 LDCM0418  CL3 HEK-293T C930(0.98)  LDD1622  [3]
 LDCM0419  CL30 HEK-293T C930(1.06)  LDD1623  [3]
 LDCM0421  CL32 HEK-293T C339(1.18); C930(1.06)  LDD1625  [3]
 LDCM0422  CL33 HEK-293T C930(1.31)  LDD1626  [3]
 LDCM0423  CL34 HEK-293T C930(1.09)  LDD1627  [3]
 LDCM0424  CL35 HEK-293T C930(1.12)  LDD1628  [3]
 LDCM0425  CL36 HEK-293T C930(1.07)  LDD1629  [3]
 LDCM0426  CL37 HEK-293T C930(0.90)  LDD1630  [3]
 LDCM0428  CL39 HEK-293T C930(0.99)  LDD1632  [3]
 LDCM0429  CL4 HEK-293T C930(1.05)  LDD1633  [3]
 LDCM0430  CL40 HEK-293T C930(1.06)  LDD1634  [3]
 LDCM0431  CL41 HEK-293T C930(1.09)  LDD1635  [3]
 LDCM0432  CL42 HEK-293T C930(1.11)  LDD1636  [3]
 LDCM0434  CL44 HEK-293T C339(1.14); C930(1.09)  LDD1638  [3]
 LDCM0435  CL45 HEK-293T C930(1.10)  LDD1639  [3]
 LDCM0436  CL46 HEK-293T C930(1.08)  LDD1640  [3]
 LDCM0437  CL47 HEK-293T C930(1.10)  LDD1641  [3]
 LDCM0438  CL48 HEK-293T C930(1.08)  LDD1642  [3]
 LDCM0439  CL49 HEK-293T C930(0.93)  LDD1643  [3]
 LDCM0440  CL5 HEK-293T C930(0.94)  LDD1644  [3]
 LDCM0441  CL50 HEK-293T C930(1.19)  LDD1645  [3]
 LDCM0443  CL52 HEK-293T C930(1.10)  LDD1646  [3]
 LDCM0444  CL53 HEK-293T C930(1.23)  LDD1647  [3]
 LDCM0445  CL54 HEK-293T C930(1.31)  LDD1648  [3]
 LDCM0447  CL56 HEK-293T C339(1.11); C930(1.13)  LDD1650  [3]
 LDCM0448  CL57 HEK-293T C930(1.21)  LDD1651  [3]
 LDCM0449  CL58 HEK-293T C930(1.11)  LDD1652  [3]
 LDCM0450  CL59 HEK-293T C930(1.09)  LDD1653  [3]
 LDCM0451  CL6 HEK-293T C930(1.17)  LDD1654  [3]
 LDCM0452  CL60 HEK-293T C930(1.00)  LDD1655  [3]
 LDCM0453  CL61 HEK-293T C930(1.02)  LDD1656  [3]
 LDCM0454  CL62 HEK-293T C930(1.06)  LDD1657  [3]
 LDCM0455  CL63 HEK-293T C930(0.92)  LDD1658  [3]
 LDCM0456  CL64 HEK-293T C930(1.17)  LDD1659  [3]
 LDCM0457  CL65 HEK-293T C930(1.10)  LDD1660  [3]
 LDCM0458  CL66 HEK-293T C930(1.17)  LDD1661  [3]
 LDCM0460  CL68 HEK-293T C339(1.09); C930(1.14)  LDD1663  [3]
 LDCM0461  CL69 HEK-293T C930(1.05)  LDD1664  [3]
 LDCM0463  CL70 HEK-293T C930(1.00)  LDD1666  [3]
 LDCM0464  CL71 HEK-293T C930(1.13)  LDD1667  [3]
 LDCM0465  CL72 HEK-293T C930(1.18)  LDD1668  [3]
 LDCM0466  CL73 HEK-293T C930(0.97)  LDD1669  [3]
 LDCM0467  CL74 HEK-293T C930(1.21)  LDD1670  [3]
 LDCM0469  CL76 HEK-293T C930(0.99)  LDD1672  [3]
 LDCM0470  CL77 HEK-293T C930(1.13)  LDD1673  [3]
 LDCM0471  CL78 HEK-293T C930(1.05)  LDD1674  [3]
 LDCM0473  CL8 HEK-293T C339(1.09); C930(1.43)  LDD1676  [3]
 LDCM0474  CL80 HEK-293T C339(1.07); C930(0.95)  LDD1677  [3]
 LDCM0475  CL81 HEK-293T C930(0.98)  LDD1678  [3]
 LDCM0476  CL82 HEK-293T C930(1.07)  LDD1679  [3]
 LDCM0477  CL83 HEK-293T C930(1.12)  LDD1680  [3]
 LDCM0478  CL84 HEK-293T C930(1.13)  LDD1681  [3]
 LDCM0479  CL85 HEK-293T C930(0.94)  LDD1682  [3]
 LDCM0480  CL86 HEK-293T C930(1.12)  LDD1683  [3]
 LDCM0481  CL87 HEK-293T C930(0.95)  LDD1684  [3]
 LDCM0482  CL88 HEK-293T C930(0.92)  LDD1685  [3]
 LDCM0483  CL89 HEK-293T C930(1.00)  LDD1686  [3]
 LDCM0484  CL9 HEK-293T C930(1.03)  LDD1687  [3]
 LDCM0485  CL90 HEK-293T C930(1.50)  LDD1688  [3]
 LDCM0487  CL92 HEK-293T C339(1.11); C930(1.08)  LDD1690  [3]
 LDCM0488  CL93 HEK-293T C930(1.08)  LDD1691  [3]
 LDCM0489  CL94 HEK-293T C930(1.07)  LDD1692  [3]
 LDCM0490  CL95 HEK-293T C930(1.31)  LDD1693  [3]
 LDCM0491  CL96 HEK-293T C930(1.00)  LDD1694  [3]
 LDCM0492  CL97 HEK-293T C930(1.04)  LDD1695  [3]
 LDCM0493  CL98 HEK-293T C930(1.05)  LDD1696  [3]
 LDCM0494  CL99 HEK-293T C930(0.87)  LDD1697  [3]
 LDCM0495  E2913 HEK-293T C930(1.06)  LDD1698  [3]
 LDCM0468  Fragment33 HEK-293T C930(0.89)  LDD1671  [3]
 LDCM0427  Fragment51 HEK-293T C930(1.14)  LDD1631  [3]
 LDCM0022  KB02 HEK-293T C930(0.90); C339(1.11)  LDD1492  [3]
 LDCM0023  KB03 HEK-293T C930(0.99); C339(0.97)  LDD1497  [3]
 LDCM0024  KB05 NUGC-3 C930(1.78)  LDD3367  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 ubiquitin-protein ligase ZNRF3 (ZNRF3) ZNRF3 family Q9ULT6
E3 ubiquitin-protein ligase MARCHF2 (MARCHF2) . Q9P0N8

The Drug(s) Related To This Target

Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bnc-102 Antibody D2ZI3H

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 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