Details of the Target

General Information of Target

Target ID LDTP12003
Target Name Ribosomal oxygenase 1 (RIOX1)
Gene Name RIOX1
Gene ID 79697
Synonyms
C14orf169; MAPJD; NO66; Ribosomal oxygenase 1; 60S ribosomal protein L8 histidine hydroxylase; Bifunctional lysine-specific demethylase and histidyl-hydroxylase NO66; EC 1.14.11.27, EC 1.14.11.79; Myc-associated protein with JmjC domain; Nucleolar protein 66; hsNO66; Ribosomal oxygenase NO66; ROX
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASRGARQRLKGSGASSGDTAPAADKLRELLGSREAGGAEHRTELSGNKAGQVWAPEGST
AFKCLLSARLCAALLSNISDCDETFNYWEPTHYLIYGEGFQTWEYSPAYAIRSYAYLLLH
AWPAAFHARILQTNKILVFYFLRCLLAFVSCICELYFYKAVCKKFGLHVSRMMLAFLVLS
TGMFCSSSAFLPSSFCMYTTLIAMTGWYMDKTSIAVLGVAAGAILGWPFSAALGLPIAFD
LLVMKHRWKSFFHWSLMALILFLVPVVVIDSYYYGKLVIAPLNIVLYNVFTPHGPDLYGT
EPWYFYLINGFLNFNVAFALALLVLPLTSLMEYLLQRFHVQNLGHPYWLTLAPMYIWFII
FFIQPHKEERFLFPVYPLICLCGAVALSALQKCYHFVFQRYRLEHYTVTSNWLALGTVFL
FGLLSFSRSVALFRGYHGPLDLYPEFYRIATDPTIHTVPEGRPVNVCVGKEWYRFPSSFL
LPDNWQLQFIPSEFRGQLPKPFAEGPLATRIVPTDMNDQNLEEPSRYIDISKCHYLVDLD
TMRETPREPKYSSNKEEWISLAYRPFLDASRSSKLLRAFYVPFLSDQYTVYVNYTILKPR
KAKQIRKKSGG
Target Bioclass
Enzyme
Family
ROX family, NO66 subfamily
Subcellular location
Nucleus, nucleolus
Function
Oxygenase that can act as both a histone lysine demethylase and a ribosomal histidine hydroxylase. Specifically demethylates 'Lys-4' (H3K4me) and 'Lys-36' (H3K36me) of histone H3, thereby playing a central role in histone code. Preferentially demethylates trimethylated H3 'Lys-4' (H3K4me3) and monomethylated H3 'Lys-4' (H3K4me1) residues, while it has weaker activity for dimethylated H3 'Lys-36' (H3K36me2). Acts as a regulator of osteoblast differentiation via its interaction with SP7/OSX by demethylating H3K4me and H3K36me, thereby inhibiting SP7/OSX-mediated promoter activation. Also catalyzes demethylation of non-histone proteins, such as CGAS: demethylation of monomethylated CGAS promotes interaction between CGAS and PARP1, followed by PARP1 inactivation. Also catalyzes the hydroxylation of 60S ribosomal protein L8 on 'His-216', thereby playing a role in ribosome biogenesis. Participates in MYC-induced transcriptional activation.
Uniprot ID
Q9H6W3
Ensemble ID
ENST00000304061.8
HGNC ID
HGNC:20968

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K480(10.00)  LDD0277  [1]
DBIA
 Probe Info  		C584(2.42)  LDD3323  [2]
AHL-Pu-1
 Probe Info  		C150(6.32)  LDD0171  [3]
Acrolein
 Probe Info  		H578(0.00); H549(0.00)  LDD0227  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		C294(0.00); C613(0.00)  LDD0038  [5]
IA-alkyne
 Probe Info  		C584(0.00); C294(0.00)  LDD0036  [5]
Lodoacetamide azide
 Probe Info  		C294(0.00); C584(0.00); C613(0.00)  LDD0037  [5]
NAIA_5
 Probe Info  		C294(0.00); C409(0.00); C613(0.00)  LDD2223  [6]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C346
 Probe Info  		15.78  LDD2007  [7]
C413
 Probe Info  		14.83  LDD2069  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA DM93 C150(6.32)  LDD0171  [3]
 LDCM0630  CCW28-3 231MFP C150(1.35)  LDD2214  [8]
 LDCM0632  CL-Sc Hep-G2 C294(20.00)  LDD2227  [6]
 LDCM0022  KB02 A204 C584(1.95)  LDD2252  [2]
 LDCM0023  KB03 A204 C584(3.61)  LDD2669  [2]
 LDCM0024  KB05 SKMEL24 C584(2.42)  LDD3323  [2]
 LDCM0109  NEM HeLa H578(0.00); H549(0.00)  LDD0227  [4]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
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 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
4 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
5 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
6 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
7 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
8 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.