Details of the Target

General Information of Target

Target ID LDTP08952
Target Name G-protein coupled receptor 161 (GPR161)
Gene Name GPR161
Gene ID 23432
Synonyms
G-protein coupled receptor 161; G-protein coupled receptor RE2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSLNSSLSCRKELSNLTEEEGGEGGVIITQFIAIIVITIFVCLGNLVIVVTLYKKSYLLT
LSNKFVFSLTLSNFLLSVLVLPFVVTSSIRREWIFGVVWCNFSALLYLLISSASMLTLGV
IAIDRYYAVLYPMVYPMKITGNRAVMALVYIWLHSLIGCLPPLFGWSSVEFDEFKWMCVA
AWHREPGYTAFWQIWCALFPFLVMLVCYGFIFRVARVKARKVHCGTVVIVEEDAQRTGRK
NSSTSTSSSGSRRNAFQGVVYSANQCKALITILVVLGAFMVTWGPYMVVIASEALWGKSS
VSPSLETWATWLSFASAVCHPLIYGLWNKTVRKELLGMCFGDRYYREPFVQRQRTSRLFS
ISNRITDLGLSPHLTALMAGGQPLGHSSSTGDTGFSCSQDSGTDMMLLEDYTSDDNPPSH
CTCPPKRRSSVTFEDEVEQIKEAAKNSILHVKAEVHKSLDSYAASLAKAIEAEAKINLFG
EEALPGVLVTARTVPGGGFGGRRGSRTLVSQRLQLQSIEEGDVLAAEQR
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family
Subcellular location
Cell projection, cilium membrane
Function
Key negative regulator of Shh signaling, which promotes the processing of GLI3 into GLI3R during neural tube development. Recruited by TULP3 and the IFT-A complex to primary cilia and acts as a regulator of the PKA-dependent basal repression machinery in Shh signaling by increasing cAMP levels, leading to promote the PKA-dependent processing of GLI3 into GLI3R and repress the Shh signaling. In presence of SHH, it is removed from primary cilia and is internalized into recycling endosomes, preventing its activity and allowing activation of the Shh signaling. Its ligand is unknown.
Uniprot ID
Q8N6U8
Ensemble ID
ENST00000367835.1
HGNC ID
HGNC:23694
ChEMBL ID
CHEMBL4523894

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT116 Deletion: p.G497AfsTer13 .
MFE319 SNV: p.M146V .
MOLT4 SNV: p.R332H .
SNU308 SNV: p.Y135H .

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  		C224(1.19)  LDD1575  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0371  CL102 HEK-293T C224(1.19)  LDD1575  [1]
 LDCM0375  CL106 HEK-293T C224(0.96)  LDD1579  [1]
 LDCM0380  CL110 HEK-293T C224(1.22)  LDD1584  [1]
 LDCM0384  CL114 HEK-293T C224(1.16)  LDD1588  [1]
 LDCM0388  CL118 HEK-293T C224(1.20)  LDD1592  [1]
 LDCM0393  CL122 HEK-293T C224(1.05)  LDD1597  [1]
 LDCM0397  CL126 HEK-293T C224(1.10)  LDD1601  [1]
 LDCM0401  CL14 HEK-293T C224(1.18)  LDD1605  [1]
 LDCM0407  CL2 HEK-293T C224(1.46)  LDD1611  [1]
 LDCM0414  CL26 HEK-293T C224(1.11)  LDD1618  [1]
 LDCM0441  CL50 HEK-293T C224(1.08)  LDD1645  [1]
 LDCM0454  CL62 HEK-293T C224(1.07)  LDD1657  [1]
 LDCM0467  CL74 HEK-293T C224(1.17)  LDD1670  [1]
 LDCM0480  CL86 HEK-293T C224(1.17)  LDD1683  [1]
 LDCM0493  CL98 HEK-293T C224(0.96)  LDD1696  [1]
 LDCM0427  Fragment51 HEK-293T C224(1.06)  LDD1631  [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