Details of the Target

General Information of Target

Target ID LDTP10649
Target Name 28S rRNA (cytosine-C(5))-methyltransferase (NSUN5)
Gene Name NSUN5
Gene ID 55695
Synonyms
NSUN5A; WBSCR20; WBSCR20A; 28S rRNA; cytosine-C(5))-methyltransferase; EC 2.1.1.-; NOL1-related protein; NOL1R; NOL1/NOP2/Sun domain family member 5; Williams-Beuren syndrome chromosomal region 20A protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTGYEARLITFGTWMYSVNKEQLARAGFYAIGQEDKVQCFHCGGGLANWKPKEDPWEQHA
KWYPGCKYLLEEKGHEYINNIHLTRSLEGALVQTTKKTPSLTKRISDTIFPNPMLQEAIR
MGFDFKDVKKIMEERIQTSGSNYKTLEVLVADLVSAQKDTTENELNQTSLQREISPEEPL
RRLQEEKLCKICMDRHIAVVFIPCGHLVTCKQCAEAVDRCPMCSAVIDFKQRVFMS
Target Bioclass
Enzyme
Family
Class I-like SAM-binding methyltransferase superfamily, RsmB/NOP family
Subcellular location
Nucleus, nucleolus
Function
S-adenosyl-L-methionine-dependent methyltransferase that specifically methylates the C(5) position of cytosine 3782 (m5C3782) in 28S rRNA. m5C3782 promotes protein translation without affecting ribosome biogenesis and fidelity. Required for corpus callosum and cerebral cortex development.
Uniprot ID
Q96P11
Ensemble ID
ENST00000252594.10
HGNC ID
HGNC:16385
ChEMBL ID
CHEMBL4802014

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
DBIA
 Probe Info  		C41(5.35)  LDD3312  [2]
AHL-Pu-1
 Probe Info  		C308(2.23)  LDD0173  [3]
4-Iodoacetamidophenylacetylene
 Probe Info  		C343(0.00); C404(0.00); C41(0.00); C146(0.00)  LDD0038  [4]
IA-alkyne
 Probe Info  		C343(0.00); C404(0.00); C146(0.00); C41(0.00)  LDD0036  [4]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [5]
Lodoacetamide azide
 Probe Info  		C343(0.00); C404(0.00); C146(0.00); C308(0.00)  LDD0037  [4]
NAIA_4
 Probe Info  		C146(0.00); C308(0.00); C404(0.00)  LDD2226  [6]
TFBX
 Probe Info  		N.A.  LDD0027  [7]
Compound 10
 Probe Info  		N.A.  LDD2216  [8]
Compound 11
 Probe Info  		N.A.  LDD2213  [8]
IPM
 Probe Info  		N.A.  LDD0005  [9]
8d
 Probe Info  		N.A.  LDD0305  [10]
AOyne
 Probe Info  		14.80  LDD0443  [11]
NAIA_5
 Probe Info  		C404(0.00); C41(0.00); C146(0.00); C234(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
C198
 Probe Info  		12.04  LDD1874  [12]
VE-P
 Probe Info  		N.A.  LDD0396  [13]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0132  15d THP-1 N.A.  LDD0305  [10]
 LDCM0026  4SU-RNA+native RNA HEK-293T C308(2.23)  LDD0173  [3]
 LDCM0156  Aniline NCI-H1299 12.48  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C308(1.47)  LDD2214  [14]
 LDCM0632  CL-Sc Hep-G2 C41(20.00); C343(1.76); C146(0.61)  LDD2227  [6]
 LDCM0625  F8 Ramos C146(1.36); C343(0.90); C308(1.52); 1.03  LDD2187  [15]
 LDCM0572  Fragment10 Ramos C146(0.66); C343(0.80); 0.94  LDD2189  [15]
 LDCM0573  Fragment11 Ramos C146(0.17); C343(0.95); C308(0.82)  LDD2190  [15]
 LDCM0574  Fragment12 Ramos C146(0.73); C343(0.78); 6.08  LDD2191  [15]
 LDCM0575  Fragment13 Ramos C146(0.93); C343(1.04)  LDD2192  [15]
 LDCM0576  Fragment14 Ramos C146(0.73); C343(0.60); C308(0.51); 3.30  LDD2193  [15]
 LDCM0579  Fragment20 Ramos C146(0.53); C343(0.61)  LDD2194  [15]
 LDCM0580  Fragment21 Ramos C146(0.78); C343(1.02)  LDD2195  [15]
 LDCM0582  Fragment23 Ramos C146(0.89); C343(1.20)  LDD2196  [15]
 LDCM0578  Fragment27 Ramos C146(0.93)  LDD2197  [15]
 LDCM0586  Fragment28 Ramos C146(0.91); C343(0.55); C308(0.83)  LDD2198  [15]
 LDCM0588  Fragment30 Ramos C146(1.06); C343(1.06); 2.05  LDD2199  [15]
 LDCM0589  Fragment31 Ramos C146(0.77); C343(0.99)  LDD2200  [15]
 LDCM0590  Fragment32 Ramos C146(1.73); C343(0.57)  LDD2201  [15]
 LDCM0468  Fragment33 Ramos C146(1.26); C343(0.80)  LDD2202  [15]
 LDCM0596  Fragment38 Ramos C146(0.70)  LDD2203  [15]
 LDCM0566  Fragment4 Ramos C146(0.94); C343(0.63); C308(0.95)  LDD2184  [15]
 LDCM0610  Fragment52 Ramos C146(0.77)  LDD2204  [15]
 LDCM0614  Fragment56 Ramos C146(1.07); C343(1.12); 1.78  LDD2205  [15]
 LDCM0569  Fragment7 Ramos C146(0.74); C343(0.59); C308(1.03); 0.85  LDD2186  [15]
 LDCM0571  Fragment9 Ramos C146(0.67); C343(0.67)  LDD2188  [15]
 LDCM0022  KB02 HEK-293T C404(1.15); C308(0.98); C146(0.92); C362(1.00)  LDD1492  [16]
 LDCM0023  KB03 HEK-293T C404(1.18); C308(1.05); C146(1.06); C362(1.06)  LDD1497  [16]
 LDCM0024  KB05 HMCB C41(5.35)  LDD3312  [2]
 LDCM0131  RA190 MM1.R C362(1.58)  LDD0304  [17]

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
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 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
5 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
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 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
8 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
9 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
10 Berberine Directly Targets the NEK7 Protein to Block the NEK7-NLRP3 Interaction and Exert Anti-inflammatory Activity. J Med Chem. 2021 Jan 14;64(1):768-781. doi: 10.1021/acs.jmedchem.0c01743. Epub 2020 Dec 1.
11 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
12 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
13 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
14 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.
15 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
16 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
17 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.