m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03092
|
[1] | |||
m6A modification
UBR7
UBR7
ALKBH5
Demethylation
: m6A sites
Direct
Inhibition
Histone modification
H2BK120ub
UBR7
KEAP1
|
|||||
| m6A Modification: | |||||
|---|---|---|---|---|---|
| m6A Regulator | RNA demethylase ALKBH5 (ALKBH5) | ERASER | |||
| m6A Target | Putative E3 ubiquitin-protein ligase UBR7 (UBR7) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Putative E3 ubiquitin-protein ligase UBR7 (UBR7) | WRITER | View Details | ||
| Regulated Target | Histone H2B lysine 120 ubiquitination (H2BK120ub) | View Details | |||
| Downstream Gene | KEAP1 | View Details | |||
| Crosstalk Relationship | m6A → Histone modification | Inhibition | |||
| Crosstalk Mechanism | m6A modification impacts directly histone modification through modulating the expression level of histone-associated enzymes | ||||
| Crosstalk Summary | Putative E3 ubiquitin-protein ligase UBR7 (UBR7) regulates Histone H2B lysine 120 ubiquitination (H2BK120ub) to bind to KEAP1 promoter through H2BK120ub monoubiquitination, thereby modulating Keap1 expression and downstream Nrf2/Bach1/HK2 signaling. Pharmaceutical and genetic inhibition of glycolytic enzymes attenuate the promoting effect of UBR7 deficiency on tumor growth. In addition, methyltransferase ALKBH5, downregulated in HCC, regulated UBR7 expression in an m6A-dependent manner. | ||||
| Responsed Disease | Liver cancer | ICD-11: 2C12 | |||
In-vitro Model |
Huh-7 | Adult hepatocellular carcinoma | Homo sapiens | CVCL_0336 | |
| MHCC97-L | Adult hepatocellular carcinoma | Homo sapiens | CVCL_4973 | ||
| In-vivo Model | HepG2 cells overexpressing or knocking out UBR7 were injected subcutaneously into nude mice. The volume of xenograft tumours was measured weekly. After 32 days, the xenograft tumour was taken out and weighed. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Kelch-like ECH-associated protein 1 (KEAP1) | 35 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| CXA10 | Phase 2 | [2] | ||
| MOA | Inactivator | |||
| External Link | ||||
| PMID28454500-Compound-8 | Patented | [3] | ||
| MOA | Modulator | |||
| Activity | IC50(RAW264.7 cells) = 1 nM | |||
| External Link | ||||
| Pyrazino[2,1-a]isoquinolin derivative 4 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-31
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-36 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Chalcone derivative 4 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-19
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| 2-hydroxybenzamide derivative 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-38
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| Vinyl sulfone derivative 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-20
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| Pyrazino[2,1-a]isoquinolin derivative 2 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-29
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| Diterpenoid derivative 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-47
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| Activity | EC50 < 500 nM | |||
| External Link | ||||
| PMID28454500-Compound-13 | Patented | [3] | ||
| MOA | Modulator | |||
| Activity | IC50 = 0.8 nM | |||
| External Link | ||||
| PMID28454500-Compound-12 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Pyrazino[2,1-a]isoquinolin derivative 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-28
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-41 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Chalcone derivative 2 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-17
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-34 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-33 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Chalcone derivative 3 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-18
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-50 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-3 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Pyridyl compound 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-15
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| Activity | IC50 = 4.3 nM | |||
| External Link | ||||
| PMID28454500-Compound-32 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-40 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-35 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-49 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-9 | Patented | [3] | ||
| MOA | Modulator | |||
| Activity | IC50(RAW264.7 cells) = 0.7 nM | |||
| External Link | ||||
| Diterpenoid derivative 2 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-48
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| Activity | EC50 < 500 nM | |||
| External Link | ||||
| PMID28454500-Compound-11 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-37 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Chalcone derivative 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-16
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| Pyrazino[2,1-a]isoquinolin derivative 3 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-30
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| 2-hydroxybenzamide derivative 2 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-39
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| PMID28454500-Compound-10 | Patented | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Trepenoid derivative 1 | Patented | [3] | ||
| Synonyms |
PMID28454500-Compound-14
Click to Show/Hide
|
|||
| MOA | Modulator | |||
| External Link | ||||
| VCB101 | Preclinical | [4] | ||
| MOA | Inactivator | |||
| External Link | ||||
| VCB102 | Preclinical | [4] | ||
| MOA | Inactivator | |||
| External Link | ||||
| 2C12: Liver cancer | 49 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| 90Y-loaded resin microspheres | Approved | [5] | ||
| External Link | ||||
| Thymalfasin | Phase 2 | [6] | ||
| Synonyms |
Zadaxin; 62304-98-7; Thymosin alpha1; Thymosin alpha 1; Thymosin alpha1 (ox); Thymosin alpha1 (human); Thymalfasin [USAN:INN]; UNII-W0B22ISQ1C; Thymosin-alpha-1; 69440-99-9; Thymosin alpha1 (cattle); C129H215N33O55; W0B22ISQ1C; Zadaxin (TN); Thymalfasin alfa 1
Click to Show/Hide
|
|||
| External Link | ||||
| Ferumoxides | Approved | [7] | ||
| Synonyms |
AMI-25; 119683-68-0; Feridex; Feridex IV; Superparamagnetic iron oxide; UNII-G6N3J05W84; Ferumoxides [USAN:USP:BAN]; CCRIS 6722; HSDB 8072; AC1O5DID; G6N3J05W84; iron(2+); iron(3+); Iron oxide crystal is inverse spinel (X-ray data); Fe(II) and Fe(III) are present (Mossbauer Spectroscopy; Physical form is a colloidal particle of nonstoichiometric
Click to Show/Hide
|
|||
| External Link | ||||
| DTI-015 | Approved | [8] | ||
| Synonyms |
Carmustine; 154-93-8; 1,3-Bis(2-chloroethyl)-1-nitrosourea; BCNU; Carmustin; Nitrumon; Carmubris; Gliadel; BiCNU; Bi CNU; Carmustinum; Bischlorethylnitrosurea; Bischlorethylnitrosourea; Carmustina; Becenun; Becenum; Bischloroethyl nitrosourea; N,N'-BIS(2-CHLOROETHYL)-N-NITROSOUREA; Bis(2-chloroethyl)nitrosourea; Urea, N,N'-bis(2-chloroethyl)-N-nitroso-; Gliadel Wafer; FDA 0345; Bischloroethylnitrosourea; SRI 1720; 1,3-Bis(2-chloroethyl)nitrosourea; BiCNU (TN); Carmustinum [INN-Latin]; Carmustina [INN-Spanish]; DTI 015; NCI-C04773; SK; Injectable carmustine, Direct Therapeutics
Click to Show/Hide
|
|||
| External Link | ||||
| Nofazinlimab | Phase 3 | [9] | ||
| Synonyms |
CS1003; EQ176
Click to Show/Hide
|
|||
| External Link | ||||
| PV-10 | Phase 3 | [10] | ||
| Synonyms |
632-69-9; Rose bengal sodium; Rose bengal disodium salt; R105 sodium; Rose-bengal (131 I) natrium; Food Red No 105, sodium salt; EINECS 211-183-3; Food Red Color No 105, sodium salt; Sel disodique de rose bengale iodee (131 I); Rose bengale (131 I) sodique [INN-French]; Rosa bengala sodica (131 I) [INN-Spanish]; Roseum bengalense (131 I) natricum [INN-Latin]; 2,4,5,7-Tetraido(m,p,o',m')tetrachlorofluorescein, disodium salt; Fluorescein, 4,5,6,7-tetrachloro-2',4',5',7'-tetraiodo-, disodium salt; Disodium
Click to Show/Hide
|
|||
| External Link | ||||
| Brivanib | Phase 3 | [11] | ||
| Synonyms |
649735-46-6; BMS-540215; Brivanib (BMS-540215); BMS 540215; UNII-DDU33B674I; Brivanib [USAN]; BMS540215; DDU33B674I; CHEMBL377300; (2R)-1-[4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]propanol; Brivanib (USAN); (2R)-1-[4-[(4-FLUORO-2-METHYL-1H-INDOL-5-YL)OXY]-5-METHYL-PYRROLO[2,1-F][1,2,4]TRIAZIN-6-YL]OXYPROPAN-2-OL; (2R)-1-({4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl}oxy)propan-2-ol
Click to Show/Hide
|
|||
| External Link | ||||
| JX-594 | Phase 3 | [12] | ||
| Synonyms |
Pexastimogene devacirepvec
Click to Show/Hide
|
|||
| External Link | ||||
| ABH001 | Phase 3 | [13] | ||
| External Link | ||||
| MTC-DOX | Phase 2/3 | [14] | ||
| Synonyms |
MTC-doxorubicin
Click to Show/Hide
|
|||
| External Link | ||||
| KD018 | Phase 2 | [15] | ||
| External Link | ||||
| Doxorubicin-eluting beads | Phase 2 | [16] | ||
| Synonyms |
DC Bead (TN)
Click to Show/Hide
|
|||
| External Link | ||||
| 32-P BioSilicon | Phase 2 | [17] | ||
| Synonyms |
BrachySil
Click to Show/Hide
|
|||
| External Link | ||||
| Cixutumumab | Phase 2 | [18] | ||
| Synonyms |
LY3012217
Click to Show/Hide
|
|||
| External Link | ||||
| [131I]-Metuximab | Phase 2 | [19] | ||
| External Link | ||||
| Darinaparsin | Phase 2 | [20] | ||
| Synonyms |
ZIO-101
Click to Show/Hide
|
|||
| External Link | ||||
| Tigatuzumab | Phase 2 | [21] | ||
| External Link | ||||
| CMC-001 | Phase 2 | [22] | ||
| Synonyms |
Manganese-based MRI contrast agent (liver tumor imaging), CMC Contrast
Click to Show/Hide
|
|||
| External Link | ||||
| OBP-301 | Phase 1/2 | [23] | ||
| External Link | ||||
| MBO7133 | Phase 1/2 | [24] | ||
| External Link | ||||
| INCB62079 | Phase 1/2 | [10] | ||
| External Link | ||||
| NV-1020 | Phase 1/2 | [25] | ||
| External Link | ||||
| DCVax-Liver | Phase 1/2 | [26] | ||
| Synonyms |
Dendritic cell-based immunotherapy (liver cancer), Northwest Biotherapeutics
Click to Show/Hide
|
|||
| External Link | ||||
| SRF388 | Phase 1 | [27] | ||
| External Link | ||||
| ET140202 | Phase 1 | [28] | ||
| External Link | ||||
| ADP-A2AFP | Phase 1 | [29] | ||
| External Link | ||||
| SM04755 | Phase 1 | [30] | ||
| External Link | ||||
| Anti-CEA CAR-T therapy | Phase 1 | [10] | ||
| External Link | ||||
| PI-166 | Phase 1 | [31] | ||
| External Link | ||||
| CRS-100 | Phase 1 | [32] | ||
| External Link | ||||
| Autologous ET1402L1-CART cells | Phase 1 | [33] | ||
| External Link | ||||
| Anti-CD133-CAR vector-transduced T cells | Phase 1 | [34] | ||
| External Link | ||||
| MRX34 | Phase 1 | [35] | ||
| External Link | ||||
| ALN-VSP | Phase 1 | [36] | ||
| External Link | ||||
| EPCAM-targeted CAR-T cells | Clinical trial | [37] | ||
| External Link | ||||
| ADI | Discontinued in Phase 3 | [38] | ||
| Synonyms |
Arginine deiminase
Click to Show/Hide
|
|||
| External Link | ||||
| GN-1140 | Discontinued in Phase 2 | [39] | ||
| External Link | ||||
| OGT-719 | Discontinued in Phase 2 | [40] | ||
| Synonyms |
OGS-719
Click to Show/Hide
|
|||
| External Link | ||||
| AFP-Scan | Discontinued in Phase 2 | [41] | ||
| External Link | ||||
| SR1078 | Preclinical | [42] | ||
| Synonyms |
1246525-60-9; SR 1078; SR-1078; N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-(trifluoromethyl)benzamide; CHEMBL3094387; N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-4-(trifluoromethyl)benzamide; N-[4-[2,2,2-Trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-4-(trifluoromethyl)benzamide; SCHEMBL4880524; C17H10F9NO2; DTXSID30591895; BCP09203; EX-A2215; 4063AH; BDBM50444350; s5775; ZINC98052696; AKOS024458390; CS-1045; NCGC00379222-02; AK547149; AS-55921; HY-14422; W-5797; SR-03000001078; SR-03000001078-1; SR-03000001078-2
Click to Show/Hide
|
|||
| External Link | ||||
| Occlusin | Preclinical | [43] | ||
| Synonyms |
Occlusin 50 Injection; Occlusin 500 injection
Click to Show/Hide
|
|||
| External Link | ||||
| HRC-201 | Terminated | [44] | ||
| Synonyms |
Hemoglobin-imaging conjugate (HepSelect), Hemosol
Click to Show/Hide
|
|||
| External Link | ||||
| 1,2,3,4,5,6-hexabromocyclohexane | Investigative | [45] | ||
| Synonyms |
1837-91-8; Benzene hexabromide; Cyclohexane, 1,2,3,4,5,6-hexabromo-; Hexabromocyclohexane; JAK2 Inhibitor II; ACMC-1BQJT; SCHEMBL459442; trans-alpha-Benzene hexabromide; CHEMBL444236; DTXSID4052687; CHEBI:93940; NSC7908; HMS3268H22; HMS3413C10; HMS3677C10; NSC-7908; ZINC1586309; ANW-23174; MFCD00059127; s5902; Cyclohexane,2,3,4,5,6-hexabromo-; AKOS015836040; 1,2,3,4,5,6-Hexabromo-cyclohexane; 1,2,3,4,5,6-Hexabromocyclohexane #; NCGC00092358-01; NCGC00092358-02; 1,2,3,4,5,6-hexakis(bromanyl)cyclohexane; A4510; FT-0633875; JAK2 Inhibitor II - CAS 1837-91-8; 1,2,3,4,5,6-Hexabromocyclohexane;NSC7908; A812818; 1,2,3,4,5,6-Hexabrom-cyclohexan (I(2)-Form); J-011778; 1,2,3,4,5,6-Hexabromocyclohexane, >=98% (HPLC); BRD-K06817181-001-01-5; Q27165694
Click to Show/Hide
|
|||
| External Link | ||||
| STP-322 | Investigative | [46] | ||
| Synonyms |
Multi-targeted siRNA therapeutic cocktail (nanoparticle, liver tumor), Sirnaomics
Click to Show/Hide
|
|||
| External Link | ||||
| AMB-8LK | Investigative | [46] | ||
| Synonyms |
Cancer therapy (monoclonal antibody), MAT Biopharma; Y90 anti-ferritin monoclonal antibody (cancer), MAT Biopharma; Yttrium-90 anti-ferritin mAb (cancer), MAT Biopharma; Yttrium-90 anti-ferritin mAb (Hodgkin's disease/pancreatic/liver cancer), MAT Biopharma; 90Y-AMB8LK mAb (cancer), MAT Biopharma; 90Y-AMB8LK monoclonal antibody (cancer), MAT Biopharma; 90Y-labelled anti-ferritin monoclonal antibody (cancer), MAT Biopharma
Click to Show/Hide
|
|||
| External Link | ||||
| MiR-34a mimics | Investigative | [46] | ||
| Synonyms |
MiR-34a mimics (liver cancer)
Click to Show/Hide
|
|||
| External Link | ||||
| P53 fusion protein | Investigative | [46] | ||
| Synonyms |
P53 fusion protein (pancreatic/liver cancer)
Click to Show/Hide
|
|||
| External Link | ||||
| OP-05 | Investigative | [46] | ||
| Synonyms |
OP-05 program (prodrug, liver tumor); OP-05 program (prodrug, liver tumor), Onco-Pharmakon
Click to Show/Hide
|
|||
| External Link | ||||
| GR-DD1 | Investigative | [46] | ||
| Synonyms |
Cytotoxin (hepatic metastasis), ERYtech
Click to Show/Hide
|
|||
| External Link | ||||
References
: m6A sites