Target Information
| Target General Information | Top | |||||
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| Target ID |
T76723
(Former ID: TTDI03485)
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| Target Name |
Protein arginine methyltransferase 3 (PRMT3)
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| Synonyms |
Protein arginine N-methyltransferase 3; Heterogeneous nuclear ribonucleoprotein methyltransferase-like protein 3; HRMT1L3
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| Gene Name |
PRMT3
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Methylates (mono and asymmetric dimethylation) the guanidino nitrogens of arginyl residues in some proteins.
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| UniProt ID | ||||||
| EC Number |
EC 2.1.1.-
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| Sequence |
MCSLASGATGGRGAVENEEDLPELSDSGDEAAWEDEDDADLPHGKQQTPCLFCNRLFTSA
EETFSHCKSEHQFNIDSMVHKHGLEFYGYIKLINFIRLKNPTVEYMNSIYNPVPWEKEEY LKPVLEDDLLLQFDVEDLYEPVSVPFSYPNGLSENTSVVEKLKHMEARALSAEAALARAR EDLQKMKQFAQDFVMHTDVRTCSSSTSVIADLQEDEDGVYFSSYGHYGIHEEMLKDKIRT ESYRDFIYQNPHIFKDKVVLDVGCGTGILSMFAAKAGAKKVLGVDQSEILYQAMDIIRLN KLEDTITLIKGKIEEVHLPVEKVDVIISEWMGYFLLFESMLDSVLYAKNKYLAKGGSVYP DICTISLVAVSDVNKHADRIAFWDDVYGFKMSCMKKAVIPEAVVEVLDPKTLISEPCGIK HIDCHTTSISDLEFSSDFTLKITRTSMCTAIAGYFDIYFEKNCHNRVVFSTGPQSTKTHW KQTVFLLEKPFSVKAGEALKGKVTVHKNKKDPRSLTVTLTLNNSTQTYGLQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: PMID22795084C1 | Ligand Info | |||||
| Structure Description | Crystal structure of protein arginine methyltransferase 3 | PDB:3SMQ | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | Yes | [2] |
| PDB Sequence |
HYGIHEEMLK
252 DKIRTESYRD262 FIYQNPHIFK272 DKVVLDVGCG282 TGILSMFAAK292 AGAKKVLGVD 302 QSEILYQAMD312 IIRLNKLEDT322 ITLIKGKIEE332 VHLPVEKVDV342 IISEWMGYFL 352 LFESMLDSVL362 YAKNKYLAKG372 GSVYPDICTI382 SLVAVSDVNK392 HADRIAFWDD 402 VYGFKMSCMK412 KAVIPEAVVE422 VLDPKTLISE432 PCGIKHIDCH442 TTSISDLEFS 452 SDFTLKITRT462 SMCTAIAGYF472 DIYFEKNCHN482 RVVFSTGPQS492 TKTHWKQTVF 502 LLEKPFSVKA512 GEALKGKVTV522 HKSLTVTLTL538 NNSTQTYGL
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| Ligand Name: SGC707 | Ligand Info | |||||
| Structure Description | Human Protein Arginine Methyltransferase 3 in complex with 1-isoquinolin-6-yl-3-[2-oxo-2-(pyrrolidin-1-yl)ethyl]urea | PDB:4RYL | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [1] |
| PDB Sequence |
HYGIHEEMLK
252 DKIRTESYRD262 FIYQNPHIFK272 DKVVLDVGCG282 TGILSMFAAK292 AGAKKVLGVD 302 QSEILYQAMD312 IIRLNKLEDT322 ITLIKGKIEE332 VHLPVEKVDV342 IISEWMGYFL 352 LFESMLDSVL362 YAKNKYLAKG372 GSVYPDICTI382 SLVAVSDVNK392 HADRIAFWDD 402 VYGFKMSCMK412 KAVIPEAVVE422 VLDPKTLISE432 PCGIKHIDCH442 TTSISDLEFS 452 SDFTLKITRT462 SMCTAIAGYF472 DIYFEKNCHN482 RVVFSTGPQS492 TKTHWKQTVF 502 LLEKPFSVKA512 GEALKGKVTV522 HKSLTVTLTL538 NNSTQTYGLQ548 |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Biological Network Descriptors
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Degree | 1 | Degree centrality | 1.07E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 1.88E-01 | Radiality | 1.32E+01 | Clustering coefficient | 0.00E+00 |
| Neighborhood connectivity | 1.26E+02 | Topological coefficient | 1.00E+00 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. | |||||
| REF 2 | An allosteric inhibitor of protein arginine methyltransferase 3. Structure. 2012 Aug 8;20(8):1425-35. | |||||
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