General Information of Target

Target ID LDTP13685
Target Name Frizzled-1 (FZD1)
Gene Name FZD1
Gene ID 8321
Synonyms
Frizzled-1; Fz-1; hFz1; FzE1
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MAAERQEALREFVAVTGAEEDRARFFLESAGWDLQIALASFYEDGGDEDIVTISQATPSS
VSRGTAPSDNRVTSFRDLIHDQDEDEEEEEGQRFYAGGSERSGQQIVGPPRKKSPNELVD
DLFKGAKEHGAVAVERVTKSPGETSKPRPFAGGGYRLGAAPEEESAYVAGEKRQHSSQDV
HVVLKLWKSGFSLDNGELRSYQDPSNAQFLESIRRGEVPAELRRLAHGGQVNLDMEDHRD
EDFVKPKGAFKAFTGEGQKLGSTAPQVLSTSSPAQQAENEAKASSSILIDESEPTTNIQI
RLADGGRLVQKFNHSHRISDIRLFIVDARPAMAATSFILMTTFPNKELADESQTLKEANL
LNAVIVQRLT
Target Bioclass
GPCR
Family
G-protein coupled receptor Fz/Smo family
Subcellular location
Cell membrane
Function
Receptor for Wnt proteins. Activated by WNT3A, WNT3, WNT1 and to a lesser extent WNT2, but apparently not by WNT4, WNT5A, WNT5B, WNT6, WNT7A or WNT7B. Contradictory results showing activation by WNT7B have been described for mouse. Functions in the canonical Wnt/beta-catenin signaling pathway. The canonical Wnt/beta-catenin signaling pathway leads to the activation of disheveled proteins, inhibition of GSK-3 kinase, nuclear accumulation of beta-catenin and activation of Wnt target genes. A second signaling pathway involving PKC and calcium fluxes has been seen for some family members, but it is not yet clear if it represents a distinct pathway or if it can be integrated in the canonical pathway, as PKC seems to be required for Wnt-mediated inactivation of GSK-3 kinase. Both pathways seem to involve interactions with G-proteins. May be involved in transduction and intercellular transmission of polarity information during tissue morphogenesis and/or in differentiated tissues (Probable).; (Microbial infection) Acts as a receptor for C.difficile toxin TcdB in the colonic epithelium.
Uniprot ID
Q9UP38
Ensemble ID
ENST00000287934.4
HGNC ID
HGNC:4038
ChEMBL ID
CHEMBL2346493

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
OPA-S-S-alkyne
 Probe Info 
K384(0.94); K273(4.28)  LDD3494  [1]
DBIA
 Probe Info 
C574(5.87)  LDD3418  [2]
IPM
 Probe Info 
C574(1.36)  LDD1702  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C574(1.36)  LDD1702  [3]
 LDCM0022  KB02 CC-LP-1 C574(1.64)  LDD2298  [2]
 LDCM0023  KB03 CC-LP-1 C574(2.61)  LDD2715  [2]
 LDCM0024  KB05 SG231 C574(5.87)  LDD3418  [2]

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 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
3 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