m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03298
|
[1], [2] | |||
Histone modification
H3K27ac
EZH2
METTL3
Direct
Enhancement
m6A modification
MPG
MPG
METTL3
Methylation
: m6A sites
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| m6A Modification: | |||||
|---|---|---|---|---|---|
| m6A Regulator | Methyltransferase-like 3 (METTL3) | WRITER | |||
| m6A Target | DNA-3-methyladenine glycosylase (ANPG/MPG) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Histone-lysine N-methyltransferase EZH2 (EZH2) | WRITER | View Details | ||
| Regulated Target | Histone H3 lysine 27 acetylation (H3K27ac) | View Details | |||
| Downstream Gene | METTL3 | View Details | |||
| Crosstalk Relationship | Histone modification → m6A | Enhancement | |||
| Crosstalk Mechanism | histone modification directly impacts m6A modification through modulating the level of m6A regulator | ||||
| Crosstalk Summary | METTL3 is required to maintain the features of GBM stem cells. When combined with TMZ, METTL3 silencing suppressed orthotopic TMZ-resistant xenograft growth in a cooperative manner. Mechanistically, TMZ induced a SOX4-mediated increase in chromatin accessibility at the METTL3 locus by promoting Histone H3 lysine 27 acetylation (H3K27ac) levels and recruiting RNA polymerase II. Moreover, METTL3 depletion affected the deposition of m6A on histone modification-related gene transcripts, such as EZH2, leading to nonsense-mediated mRNA decay. Two critical DNA repair genes (MGMT and DNA-3-methyladenine glycosylase (ANPG/MPG)) were m6A-modified by METTL3, whereas inhibited by METTL3 silencing or DAA-mediated total methylation inhibition, which is crucial for METTL3-improved temozolomide resistance in glioblastoma cells. | ||||
| Responsed Disease | Brain cancer | ICD-11: 2A00 | |||
| Responsed Drug | Temozolomide | ||||
| Pathway Response | Nucleotide excision repair | hsa03420 | |||
| Cell Process | DNA repair | ||||
In-vitro Model |
U-251MG | Astrocytoma | Homo sapiens | CVCL_0021 | |
| U-87MG ATCC | Glioblastoma | Homo sapiens | CVCL_0022 | ||
| In-vivo Model | Six-week-old female BALB/c nude mice were purchased from the Model Animal Research Center of Nanjing University and housed in individually ventilated micro-isolator cages under a 12 h dark/light cycle. Nude mice were divided into four groups of six mice each. After deep anesthesia, a 27-gauge needle was used to drill a burrhole into the skull 0.5 mm anterior and 2 mm lateral to the bregma. A 10 μ L gas-tight syringe (Hamilton) was then used to inject 10 μ L of the U87 MG-TMZ_R-luc cell suspension in the striatum at a depth of 3 mm from the dural surface. One week after the injection of the tumor cells, 40 mg/kg/day of TMZ in saline was administered for over 2 weeks by intraperitoneal injection. During TMZ treatment, a Xenogen IVIS Spectrum system was used to monitor the tumor growth. At the end point, brain tissues were dissected from the mice models and measured the length (a) and width (b) of the tumors. Tumor volume was calculated by the formula V = ab2/2. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Histone-lysine N-methyltransferase EZH2 (EZH2) | 74 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Tazemetostat | Approved | [3] | ||
| Synonyms |
EPZ-6438; 1403254-99-8; EPZ6438; UNII-Q40W93WPE1; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; Q40W93WPE1; EPZ 6438; E7438; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | Ki = 2.5 nM | |||
| External Link | ||||
| DS-3201b | Phase 2 | [4] | ||
| Synonyms |
Valemetostat; 1809336-39-7; UNII-60RD0234VE; 60RD0234VE; 1809336-39-7 (free base); DS-3201; (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide; Valemetostat 2HCl; Valemetostat [INN]; Valemetostat (DS-3201); CHEMBL4597193; EZH1/2 inhibitor DS-3201; SCHEMBL18393626; SCHEMBL18393627; SCHEMBL18639210; EX-A3423; DS3201; NSC813381; s8926; NSC-813381; HY-109108; CS-0039740; D11551
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| CPI-1205 | Phase 1/2 | [5] | ||
| Synonyms |
HPODOLXTMDHLLC-QGZVFWFLSA-N; 1621862-70-1; UNII-455J2479FY; CPI1205; CPI 1205; 455J2479FY; (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide; GTPL9115; SCHEMBL17329268; MolPort-044-560-382; KS-000006BA; EX-A1068; s8353; AKOS030628484; ZINC220982768; CS-7648; compound 13 [PMID: 27739677]; HY-100021; J3.556.402K; N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| SHR2554 | Phase 1/2 | [6] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CPI-0209 | Phase 1/2 | [7] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| GSK2816126 | Phase 1 | [8] | ||
| Synonyms |
GSK 126; GSK-126
Click to Show/Hide
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| MOA | Modulator | |||
| Activity | Ki = 0.5 nM | |||
| External Link | ||||
| PF-06821497 | Phase 1 | [9] | ||
| Synonyms |
UNII-S4L4MM20B6; S4L4MM20B6; CHEMBL4080228; PF06821497; 1844849-10-0; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one; SCHEMBL17330426; GTPL10516; BDBM50246967; NSC800019; DB14799; HY-101571A; NSC-800019; compound 23a [PMID: 29211475]; CS-0092626; Q29209799; 1(2H)-Isoquinolinone, 5,8-dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one; CJD
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| DS-3201 | Phase 1 | [5] | ||
| Synonyms |
QTGYNKYZRZATJB-UHFFFAOYSA-N; 701899-63-0; 2-(2-(2-Methyl-1H-imidazol-5-yl)ethyl)isoindoline-1,3-dione; 2-(2-(2-Methyl-1H-imidazol-5-yl)-ethyl)isoindoline-1,3-dione; SCHEMBL7743461; MolPort-035-945-474; MolPort-035-690-353; ZINC98086069; AKOS024459002; AKOS024262663; MCULE-2708350770; FCH4077443; AK158834; AX8292467; ST2403812; 2-[2-(2-methyl-1H-imidazol-5-yl)ethyl]-2,3-dihydro-1H-isoindole-1,3-dione
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| HH2853 | Phase 1 | [10] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-33 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bI | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-35 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| PMID28394193-Compound-54 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-24 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-27 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-25 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-50 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-47 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2 nM; Ki < 1 nM | |||
| External Link | ||||
| PMID28394193-Compound-21 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-41 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-53 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 80 nM | |||
| External Link | ||||
| PMID28394193-Compound-Figure5aVIII | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-38 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-51 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-31 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 20 nM | |||
| External Link | ||||
| PMID28394193-Compound-42 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-15 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-52 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-32 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 500 nM | |||
| External Link | ||||
| PMID28394193-Compound-23 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-29 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-30 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 16 nM | |||
| External Link | ||||
| PMID28394193-Compound-39 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-49 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-43 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-40 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bIII | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-36 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 316 nM | |||
| External Link | ||||
| PMID28394193-Compound-28 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 32 nM | |||
| External Link | ||||
| PMID28394193-Compound-22 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-18 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-16 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-44 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-20 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-19 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-37 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bII | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-26 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-17 | Patented | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-34 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-56 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.93 nM | |||
| External Link | ||||
| PMID28394193-Compound-46 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PMID28394193-Compound-57 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.45 nM | |||
| External Link | ||||
| PMID28394193-Compound-14 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21900 nM | |||
| External Link | ||||
| PMID28394193-Compound-12 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| PMID26882240-Compound-1 | Patented | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-55 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8.13 nM | |||
| External Link | ||||
| PMID28394193-Compound-45 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 168000 nM | |||
| External Link | ||||
| PMID28394193-Compound-13 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1470 nM | |||
| External Link | ||||
| EPZ005687 | Investigative | [13] | ||
| Synonyms |
EPZ-005687; EPZ 005687
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| EI1 | Investigative | [14] | ||
| Synonyms |
KB-145943
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| MOA | Inhibitor | |||
| External Link | ||||
| UNC1999 | Investigative | [15] | ||
| Synonyms |
UNC 1999; UNC-1999
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| MOA | Inhibitor | |||
| External Link | ||||
| MS1943 | Investigative | [6] | ||
| Synonyms |
2225938-17-8; SCHEMBL21271666; EX-A3962; s8918; HY-133129; CS-0112146; 6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide; 6-(6-(4-(2-(2-(Adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide
Click to Show/Hide
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| MOA | Degrader | |||
| External Link | ||||
| GSK343 | Investigative | [16] | ||
| Synonyms |
compound 6 [PMID 24900432]; GSK 343
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 174 nM | |||
| External Link | ||||
| PMID28394193-Compound-11 | Patented | [17] | ||
| External Link | ||||
| PMID28394193-Compound-10 | Patented | [17] | ||
| External Link | ||||
| PMID28394193-Compound-14 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21900 nM | |||
| External Link | ||||
| PMID28394193-Compound-12 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| PMID28394193-Compound-13 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1470 nM | |||
| External Link | ||||
| PMID28394193-Compound-56 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.93 nM | |||
| External Link | ||||
| PMID28394193-Compound-46 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PMID28394193-Compound-57 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.45 nM | |||
| External Link | ||||
| PMID28394193-Compound-55 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8.13 nM | |||
| External Link | ||||
| PMID28394193-Compound-45 | Patented | [11] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 168000 nM | |||
| External Link | ||||
| 2A00: Brain cancer | 53 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Zinostatin stimalamer | Approved | [18] | ||
| Synonyms |
Smancs (TN)
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| External Link | ||||
| Motexafin gadolinium | Approved | [19] | ||
| Synonyms |
Xcytrin; Gadolinium texaphyrin; GdT2B2; GD-Tex; Motexafin gadolinium (USAN); PCI-0120; Xcytrin (TN)
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| External Link | ||||
| Lomustine | Approved | [20] | ||
| Synonyms |
Belustine; CCNU; CINU; Cecenu; CeeNU; Chloroethylcyclohexylnitrosourea; Lomustina; Lomustinum; Bristol Myers Squibb Brand of Lomustine; CCNU [Chloroethyl nitrosoureas]; Cyclohexyl chloroethyl nitrosourea; Lomustine medac Brand; Medac Brand of Lomustine; Rhone Poulenc Rorer Brand of Lomustine; OR5087; RB 1509; SRI 2200; Bristol-Myers Squibb Brand of Lomustine; CeeNU (TN); Lomustina [INN-Spanish]; Lomustinum [INN-Latin]; NPFAPI-06; Rhone-Poulenc Rorer Brand of Lomustine; CeeNU, CCNU, Lomustine; Lomustine (USAN/INN); Lomustine [USAN:BAN:INN]; N-(2-Chloroethyl)-N'-cyclohexyl-N-nitrosourea; (Chloro-2-ethyl)-1-cyclohexyl-3-nitrosourea; (Cloro-2-etil)-1-cicloesil-3-nitrosourea; (Cloro-2-etil)-1-cicloesil-3-nitrosourea [Italian];1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea; 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea [Chloroethyl nitrosoureas]; 1-(2-Chloroethyl)-3-cyclohexylnitrosourea
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| Borocaptate sodium B 10 | Approved | [18] | ||
| External Link | ||||
| DTI-015 | Approved | [21] | ||
| 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
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| Prinomastat | Approved | [22] | ||
| Synonyms |
AG-3354; AG-3362; Prinomastat (USAN/INN); (3S)-N-hydroxy-2,2-dimethyl-4-(4-pyridin-4-yloxyphenyl)sulfonylthiomorpholine-3-carboxamide
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| INO-1001 | Phase 3 | [23] | ||
| Synonyms |
Hypoxanthine arabinoside; LT00454797; 9-[(3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H-purin-6-one
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| GliAtak | Phase 3 | [24] | ||
| Synonyms |
GliAtak (TN)
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| SOT-107 | Phase 3 | [25] | ||
| Synonyms |
TransMID
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| ICT-107 | Phase 3 | [26] | ||
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| Cintredekin besudotox | Phase 3 | [27] | ||
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| Rindopepimut | Phase 3 | [28] | ||
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| DCVax-Ovarian | Phase 3 | [29] | ||
| Synonyms |
DCVax-L; Dendritic cell-based immunotherapy (ovarian cancer), Northwest Biotherapeutics
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| DCVax-Brain | Phase 3 | [30] | ||
| Synonyms |
Dendritic cell-based immunotherapy (brain cancer), Northwest Biotherapeutics
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| TVI-Brain-1 | Phase 2/3 | [31] | ||
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| NLG8189 | Phase 2/3 | [5] | ||
| Synonyms |
1-Methyl-D-tryptophan; Indoximod; 110117-83-4; D-Tryptophan, 1-methyl-; D-1MT; Indoximod (NLG-8189); D-1-methyltryptophan; UNII-TX5CYN1KMZ; D-(+)-1-Methyltryptophan; TX5CYN1KMZ; (R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid; (2R)-2-amino-3-(1-methylindol-3-yl)propanoic acid; NSC-721782; (2R)-2-amino-3-(1-methyl-3-indolyl)propanoic acid; 1-MT; (2R)-2-azanyl-3-(1-methylindol-3-yl)propanoic acid; (2R)-2-amino-3-(1-methyl-1H-indol-3-yl)propanoic acid; D-l-Methyltryptophan; Indoximod [USAN:INN]; NLG-8189; NLG 8189
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| Synthetic survivin peptide vaccine | Phase 2 | [32] | ||
| External Link | ||||
| Fresolimumab | Phase 2 | [33] | ||
| Synonyms |
GC-1008
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| DNX-2401 | Phase 2 | [34] | ||
| Synonyms |
Tasadenoturev
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| TVI-Brain-1 cancer vaccine | Phase 2 | [35] | ||
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| PDT with Photofrin | Phase 2 | [5] | ||
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| F18-ML-10 | Phase 2 | [36] | ||
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| PT2385 | Phase 2 | [37] | ||
| Synonyms |
ONBSHRSJOPSEGS-INIZCTEOSA-N; PT-2385; UNII-6O16716DXP; 1672665-49-4; 6O16716DXP; SCHEMBL16555810; ZINC230453533; AKOS030526641; HY-12867; PT2385,1672665-49-4, PT 2385,PT-2385; Benzonitrile, 3-(((1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl)oxy)-5-fluoro-; 3-{[(1s)-2,2-Difluoro-1-Hydroxy-7-(Methylsulfonyl)-2,3-Dihydro-1h-Inden-4-Yl]oxy}-5-Fluorobenzonitrile; 3-(((1S)-2,2-Difluoro-1-hydroxy-7-methanesulfonyl-2,3-dihydro-1hinden-4-yl)oxy)-5-fluorobenzonitrile; 79A
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| ABT-414 | Phase 2 | [38] | ||
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| CLR1404-I-124 | Phase 1/2 | [39] | ||
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| DM-CHOC-PEN | Phase 2 | [40] | ||
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| L-alanosine | Phase 2 | [41] | ||
| Synonyms |
SDX-102
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| APX005M | Phase 2 | [5] | ||
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| WP-1066 | Phase 1/2 | [35] | ||
| Synonyms |
WP1066; 857064-38-1; (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide; WP 1066; UNII-63V8AIE65T; 63V8AIE65T; AK-99218; C17H14BrN3O; (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide; MLS006010178; SCHEMBL1315826; QCR-16; SCHEMBL1315831; GTPL7972; CHEMBL1923234; EX-A760; AOB1497; DTXSID50235007; MolPort-044-723-708; MolPort-023-219-149; ZINC13983221; AKOS016007983; WP1066/WP-1066; CS-2736; DB12679; 2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-((1S)-1-phenylethyl)-, (2E)-; HY-15312
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| Anti-EGFRvIII CAR transduced PBL | Phase 1/2 | [42] | ||
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| RG6156 | Phase 1 | [43] | ||
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| rhenium-186 | Phase 1 | [44] | ||
| Synonyms |
(~186~Re)Rhenium; 14998-63-1; 186Re; DTXSID60933825; Q18882928; RHENIUM (186-RE); Rhenium Re-186; Rhenium, isotope of mass 186; Rhenium-186; RHENIUM-186 [WHO-DD]; UNII-ZU7F1ET6TM; ZU7F1ET6TM
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| IGV-001 | Phase 1 | [45] | ||
| External Link | ||||
| DA-3607 | Phase 1 | [46] | ||
| Synonyms |
Ad-stTRAIL; TRAIL adenoviral gene therapy (cancer), Dong-A
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| DC/I540/KLH vaccine | Phase 1 | [47] | ||
| Synonyms |
HTERT:540-548; Telomerase: 540-548 peptide vaccine; DC/I540/KLH vaccine (cancer); Dendritic cell/hTERT peptide I540/keyhole limpet hemocyanin vaccine, Dana-Farber; DC/I540/KLH vaccine (cancer), Dana-Farber
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| KX2-361 | Phase 1 | [48] | ||
| Synonyms |
KX-02
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| MR1-1 | Phase 1 | [49] | ||
| Synonyms |
MR1-1KDEL; EGFR-specific immunotoxin, IVAX; Anticancer immunotoxin (EGFR-specific), IVAX
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| INdoximod + temozolomide | Phase 1 | [35] | ||
| External Link | ||||
| Anti-CD133-CAR vector-transduced T cells | Phase 1 | [50] | ||
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| 8H9 | Phase 1 | [51] | ||
| External Link | ||||
| CC-8490 | Phase 1 | [52] | ||
| External Link | ||||
| Sitimagene ceradenovec | Discontinued in Phase 3 | [53] | ||
| Synonyms |
Cerepro; EG-009; HSV thymidine kinase gene therapy, Ark
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| Ranagengliotucel-T | Discontinued in Phase 3 | [54] | ||
| Synonyms |
Glionix; Brain tumor vaccine, NovaRx; Antisense (TGFbeta) brain tumor vaccine, NovaRx
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| Oncolysin S | Discontinued in Phase 2 | [55] | ||
| Synonyms |
N901-bR
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| Labradimil | Discontinued in Phase 2 | [56] | ||
| Synonyms |
Cereport; Lobradimil; Receptor mediated permeabilizer; RMP 7; DRG-0182; RMP-7; N2-((S)-2-(L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-L-prolinamido)-3-(p-methoxyphenyl)propyl)-L-arginine; (S-(R*,R*))-L-Arginyl-L-prolyl-trans-4-hydroxy-L-prolyl-3-(2-thienyl)-L-alanylglycyl-L-seryl-N-(2-((4-((aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-L-prolinamide
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| Brain tumor vaccine | Discontinued in Phase 1 | [57] | ||
| Synonyms |
Brain cancer vaccine, IRC; Brain tumor vaccine, IRC; IR-850; Established cancer cell line therapy (brain cancer), IRC; GM-CSF vaccine (brain cancer), IRC
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| PCNU | Terminated | [58] | ||
| Synonyms |
NSC-95466
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| 131I-81C6 | Terminated | [59] | ||
| Synonyms |
Neuradiab; MAb-81C6; Iodine-131-81C6; Astatine-211-MAb-81C6; Iodine-131-MAb-81C6; Iodine-131-ch-81C6; Iodine-131-ch-81C6-F(ab)2; 211At-MAb-81C6
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| NSD-551 | Terminated | [60] | ||
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BK channel activator (cancer), NeuroSearch/TopoTarget
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| AGT-2000 | Investigative | [61] | ||
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Gene therapy (intravenous, brain cancer), ArmaGen
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| NV.XOD.09 | Investigative | [62] | ||
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| EDP-19 | Investigative | [62] | ||
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SiRNA (convection-enhanced delivery, brain tumor), Sheba Medical Center/BioLineRx
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| MIQ-004 | Investigative | [62] | ||
| Synonyms |
M-IQ-004
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References
: m6A sites