Details of the Target

General Information of Target

Target ID LDTP07331
Target Name E3 ubiquitin-protein ligase RNF43 (RNF43)
Gene Name RNF43
Gene ID 54894
Synonyms
E3 ubiquitin-protein ligase RNF43; EC 2.3.2.27; RING finger protein 43; RING-type E3 ubiquitin transferase RNF43
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSGGHQLQLAALWPWLLMATLQAGFGRTGLVLAAAVESERSAEQKAIIRVIPLKMDPTGK
LNLTLEGVFAGVAEITPAEGKLMQSHPLYLCNASDDDNLEPGFISIVKLESPRRAPRPCL
SLASKARMAGERGASAVLFDITEDRAAAEQLQQPLGLTWPVVLIWGNDAEKLMEFVYKNQ
KAHVRIELKEPPAWPDYDVWILMTVVGTIFVIILASVLRIRCRPRHSRPDPLQQRTAWAI
SQLATRRYQASCRQARGEWPDSGSSCSSAPVCAICLEEFSEGQELRVISCLHEFHRNCVD
PWLHQHRTCPLCMFNITEGDSFSQSLGPSRSYQEPGRRLHLIRQHPGHAHYHLPAAYLLG
PSRSAVARPPRPGPFLPSQEPGMGPRHHRFPRAAHPRAPGEQQRLAGAQHPYAQGWGLSH
LQSTSQHPAACPVPLRRARPPDSSGSGESYCTERSGYLADGPASDSSSGPCHGSSSDSVV
NCTDISLQGVHGSSSTFCSSLSSDFDPLVYCSPKGDPQRVDMQPSVTSRPRSLDSVVPTG
ETQVSSHVHYHRHRHHHYKKRFQWHGRKPGPETGVPQSRPPIPRTQPQPEPPSPDQQVTR
SNSAAPSGRLSNPQCPRALPEPAPGPVDASSICPSTSSLFNLQKSSLSARHPQRKRRGGP
SEPTPGSRPQDATVHPACQIFPHYTPSVAYPWSPEAHPLICGPPGLDKRLLPETPGPCYS
NSQPVWLCLTPRQPLEPHPPGEGPSEWSSDTAEGRPCPYPHCQVLSAQPGSEEELEELCE
QAV
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
ZNRF3 family
Subcellular location
Cell membrane
Function
E3 ubiquitin-protein ligase that acts as a negative regulator of the Wnt signaling pathway by mediating the ubiquitination, endocytosis and subsequent degradation of Wnt receptor complex components Frizzled. Acts on both canonical and non-canonical Wnt signaling pathway. Along with RSPO2 and ZNRF3, constitutes a master switch that governs limb specification.
TTD ID
T45968
Uniprot ID
Q68DV7
DrugMap ID
TTD91BL
Ensemble ID
ENST00000407977.7
HGNC ID
HGNC:18505

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 Deletion: p.G659VfsTer41 .
COLO800 SNV: p.S124N .
HCT116 Deletion: p.R117AfsTer41 .
HCT15 Deletion: p.G659VfsTer41
SNV: p.L214M		 .
HT115 SNV: p.G447E .
Ishikawa (Heraklio) 02 ER Deletion: p.G659VfsTer41 .
KMRC3 SNV: p.S362A .
LS123 Deletion: p.R221PfsTer197 .
LS180 SNV: p.K108E .
MCAS Deletion: p.L276GfsTer5 .
MOLT4 SNV: p.G102E; p.A115P .
NCIH2172 Substitution: p.D300F .
NCIH716 Deletion: p.H472QfsTer30
SNV: p.Y457Ter		 .
OVCAR5 SNV: p.W302C .
RKO Deletion: p.G659VfsTer41
SNV: p.H549N		 .
SH4 SNV: p.P260S .
SNU423 SNV: p.I485V .
TOV21G Deletion: p.G659VfsTer41
SNV: p.C298Y		 .
UACC257 SNV: p.V107L .

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
CY-1
 Probe Info  		N.A.  LDD0246  [1]
IPM
 Probe Info  		N.A.  LDD0147  [2]

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
Ubiquitin-conjugating enzyme E2 D2 (UBE2D2) Ubiquitin-conjugating enzyme family P62837
Ubiquitin-conjugating enzyme E2 D3 (UBE2D3) Ubiquitin-conjugating enzyme family P61077
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
A-kinase anchor protein 8-like (AKAP8L) AKAP95 family Q9ULX6
Polyubiquitin-B (UBB) Ubiquitin family P0CG47

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rnf43-721 . D01EXL

References

1 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
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