General Information of Target

Target ID LDTP07790
Target Name E3 ubiquitin-protein ligase Arkadia (RNF111)
Gene Name RNF111
Gene ID 54778
Synonyms
E3 ubiquitin-protein ligase Arkadia; EC 2.3.2.27; RING finger protein 111; hRNF111; RING-type E3 ubiquitin transferase Arkadia
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSQWTPEYNELYTLKVDMKSEIPSDAPKTQESLKGILLHPEPIGAAKSFPAGVEMINSKV
GNEFSHLCDDSQKQEKEMNGNQQEQEKSLVVRKKRKSQQAGPSYVQNCVKENQGILGLRQ
HLGTPSDEDNDSSFSDCLSSPSSSLHFGDSDTVTSDEDKEVSVRHSQTILNAKSRSHSAR
SHKWPRTETESVSGLLMKRPCLHGSSLRRLPCRKRFVKNNSSQRTQKQKERILMQRKKRE
VLARRKYALLPSSSSSSENDLSSESSSSSSTEGEEDLFVSASENHQNNPAVPSGSIDEDV
VVIEASSTPQVTANEEINVTSTDSEVEIVTVGESYRSRSTLGHSRSHWSQGSSSHASRPQ
EPRNRSRISTVIQPLRQNAAEVVDLTVDEDEPTVVPTTSARMESQATSASINNSNPSTSE
QASDTASAVTSSQPSTVSETSATLTSNSTTGTSIGDDSRRTTSSAVTETGPPAMPRLPSC
CPQHSPCGGSSQNHHALGHPHTSCFQQHGHHFQHHHHHHHTPHPAVPVSPSFSDPACPVE
RPPQVQAPCGANSSSGTSYHEQQALPVDLSNSGIRSHGSGSFHGASAFDPCCPVSSSRAA
IFGHQAAAAAPSQPLSSIDGYGSSMVAQPQPQPPPQPSLSSCRHYMPPPYASLTRPLHHQ
ASACPHSHGNPPPQTQPPPQVDYVIPHPVHAFHSQISSHATSHPVAPPPPTHLASTAAPI
PQHLPPTHQPISHHIPATAPPAQRLHPHEVMQRMEVQRRRMMQHPTRAHERPPPHPHRMH
PNYGHGHHIHVPQTMSSHPRQAPERSAWELGIEAGVTAATYTPGALHPHLAHYHAPPRLH
HLQLGALPLMVPDMAGYPHIRYISSGLDGTSFRGPFRGNFEELIHLEERLGNVNRGASQG
TIERCTYPHKYKKVTTDWFSQRKLHCKQDGEEGTEEDTEEKCTICLSILEEGEDVRRLPC
MHLFHQVCVDQWLITNKKCPICRVDIEAQLPSES
Target Bioclass
Enzyme
Family
Arkadia family
Subcellular location
Nucleus
Function
E3 ubiquitin-protein ligase. Required for mesoderm patterning during embryonic development. Acts as an enhancer of the transcriptional responses of the SMAD2/SMAD3 effectors, which are activated downstream of BMP. Acts by mediating ubiquitination and degradation of SMAD inhibitors such as SMAD7, inducing their proteasomal degradation and thereby enhancing the transcriptional activity of TGF-beta and BMP. In addition to enhance transcription of SMAD2/SMAD3 effectors, also regulates their turnover by mediating their ubiquitination and subsequent degradation, coupling their activation with degradation, thereby ensuring that only effectors 'in use' are degraded. Activates SMAD3/SMAD4-dependent transcription by triggering signal-induced degradation of SNON isoform of SKIL. Associates with UBE2D2 as an E2 enzyme. Specifically binds polysumoylated chains via SUMO interaction motifs (SIMs) and mediates ubiquitination of sumoylated substrates. Catalyzes 'Lys-63'-linked ubiquitination of sumoylated XPC in response to UV irradiation, promoting nucleotide excision repair. Mediates ubiquitination and degradation of sumoylated PML. The regulation of the BMP-SMAD signaling is however independent of sumoylation and is not dependent of SUMO interaction motifs (SIMs).
Uniprot ID
Q6ZNA4
Ensemble ID
ENST00000348370.9
HGNC ID
HGNC:17384

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 
C108(1.81)  LDD3369  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0369  CL100 HEK-293T C68(1.08)  LDD1573  [2]
 LDCM0373  CL104 HEK-293T C68(0.94)  LDD1577  [2]
 LDCM0377  CL108 HEK-293T C68(1.01)  LDD1581  [2]
 LDCM0382  CL112 HEK-293T C68(0.92)  LDD1586  [2]
 LDCM0386  CL116 HEK-293T C68(1.01)  LDD1590  [2]
 LDCM0391  CL120 HEK-293T C68(0.91)  LDD1595  [2]
 LDCM0395  CL124 HEK-293T C68(0.85)  LDD1599  [2]
 LDCM0399  CL128 HEK-293T C68(0.86)  LDD1603  [2]
 LDCM0403  CL16 HEK-293T C68(0.91)  LDD1607  [2]
 LDCM0416  CL28 HEK-293T C68(1.18)  LDD1620  [2]
 LDCM0429  CL4 HEK-293T C68(0.74)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C68(1.03)  LDD1634  [2]
 LDCM0443  CL52 HEK-293T C68(1.04)  LDD1646  [2]
 LDCM0456  CL64 HEK-293T C68(0.90)  LDD1659  [2]
 LDCM0469  CL76 HEK-293T C68(1.10)  LDD1672  [2]
 LDCM0482  CL88 HEK-293T C68(0.92)  LDD1685  [2]
 LDCM0022  KB02 HEK-293T C68(0.92)  LDD1492  [2]
 LDCM0023  KB03 HEK-293T C68(0.72)  LDD1497  [2]
 LDCM0024  KB05 OAW-42 C108(1.81)  LDD3369  [1]

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 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