Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT00084
[1], [2], [3]
m6A modification ADARB1 ADARB1 YTHDF2 : m6A sites Direct Inhibition RNA modification GRIA2 GRIA2 ADARB1 Methylation : modification sites
m6A Modification:
m6A Regulator YTH domain-containing family protein 2 (YTHDF2) READER
m6A Target Double-stranded RNA-specific editase 1 (ADARB1)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type RNA modification (RNAMod)  >> Adenosine-to-Inosine editing (A-to-I)
Epigenetic Regulator Double-stranded RNA-specific editase 1 (ADARB1) WRITER View Details
Regulated Target Glutamate ionotropic receptor AMPA type subunit 2 (GRIA2) View Details
Crosstalk Relationship m6A  →  A-to-I Inhibition
Crosstalk Mechanism m6A modification directly impacts RNA modification through modulating the expression level of RNA modification regulator
Crosstalk Summary YTHDF2 recognizes the m6A methylation sites and prevents Double-stranded RNA-specific editase 1 (ADARB1) dependent A-to-I RNA editing of Glutamate ionotropic receptor AMPA type subunit 2 (GRIA2).
Responsed Drug E-2007
In-vitro Model
A-172 Glioblastoma Homo sapiens CVCL_0131
HeLa Endocervical adenocarcinoma Homo sapiens CVCL_0030
SH-SY5Y Neuroblastoma Homo sapiens CVCL_0019
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Glutamate ionotropic receptor AMPA type subunit 2 (GRIA2) 6 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name E-2007 Approved [4]
Synonyms
Perampanel; E 2007; Perampanel (USAN); 2-(2-oxo-1-phenyl-5-pyridin-2-yl-pyridin-3-yl)benzonitrile; 3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one
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MOA Inhibitor
External Link
 Compound Name Paliroden Phase 2 [5]
Synonyms
SR-57667; SR-57667B
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MOA Modulator
External Link
 Compound Name ATPO Investigative [6]
Synonyms
252930-37-3; (R,S)-2-Amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid; 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-1,2-oxazol-4-yl]propanoic acid; ATPO, solid; AC1NECDZ; Lopac0_000092; SCHEMBL4318475; CHEMBL265301; GTPL4141; DTXSID70404915; MolPort-003-940-289; HMS3261F20; HMS3260C06; Tox21_500589; Tox21_500092; MFCD03452828; LP00092; LP00589; CCG-204187; NCGC00261274-01; NCGC00260777-01; NCGC00015093-05; NCGC00015093-02; NCGC00093594-01; NCGC00015093-04; NCGC00093594-02; NCGC00015093-03; EU-0100092; A 7845
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MOA Antagonist
External Link
 Compound Name (S)-5-fluorowillardiine Investigative [6]
Synonyms
5-Fluorowillardiine; (S)-(-)-5-fluorowillardiine; 140187-23-1; FLUORO-WILLARDIINE; (S)-F-Willardiine; 2-AMINO-3-(5-FLUORO-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YL)-PROPIONIC ACID; CHEMBL123132; CHEBI:42549; 3-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-L-alanine; (S)-alpha-Amino-5-fluoro-3,4-dihydro-2,4-dioxo-1(2H)-pyrimmidinepropanoic acid; 3-(5-fluorouracil-1-yl)-L-alanine; (2S)-2-amino-3-(5-fluoro-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)propanoic acid; (S)-(-)-5-fluorowillardine
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MOA Agonist
Activity Ki = 25.1 nM
External Link
 Compound Name [3H]AMPA Investigative [6]
Synonyms
alpha-AMINO-3-HYDROXY-5-METHYL-4-ISOXAZOLEPROPIONIC ACID; ampa; 74341-63-2; 77521-29-0; (RS)-AMPA; AMPA (pharmaceutical); CHEMBL13378; CHEBI:34018; 4-Isoxazolepropanoic acid, alpha-amino-2,3-dihydro-5-methyl-3-oxo-; gamma-Amino-3-hydroxy-5-methylisoxazole-4-propionic acid; dl-alpha-Amino-3-hydroxy-5-methylisoxazole-4-propionic acid; (+-)-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; D,L-alpha-Amino-3-hydroxy-5-methylisoxazole-4-propionic acid
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MOA Agonist
External Link
 Compound Name [3H]CNQX Investigative [6]
Synonyms
6-Cyano-7-nitroquinoxaline-2,3-dione; CNQX; 115066-14-3; 7-Nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-carbonitrile; UNII-6OTE87SCCW; FG 9065; 6OTE87SCCW; FG-9065; 6-Cyano-2,3-dihydroxy-7-nitroquinoxaline; CHEBI:34468; 1,4-dihydro-2,3-dihydroxy-7-nitro-6-quinoxalinecarbonitrile; 7-nitro-2,3-dioxo-1,4-dihydroquinoxaline-6-carbonitrile; 6-Quinoxalinecarbonitrile, 1,2,3,4-tetrahydro-7-nitro-2,3-dioxo-; ST50405216; 2,3-dihydroxy-7-nitro-6-quinoxalinecarbonitrile; FG9065; AC1MWAKF; Tocris-0190; Biomol-NT_000200
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MOA Antagonist
External Link
References
Ref 1 N6-methyladenosine promotes induction of ADAR1-mediated A-to-I RNA editing to suppress aberrant antiviral innate immune responses. PLoS Biol. 2021 Jul 29;19(7):e3001292. doi: 10.1371/journal.pbio.3001292. eCollection 2021 Jul.
Ref 2 Determination of editors at the novel A-to-I editing positions. Neurosci Res. 2008 Jun;61(2):201-6. doi: 10.1016/j.neures.2008.02.009. Epub 2008 Mar 13.
Ref 3 ADAR2-dependent A-to-I RNA editing in the extracellular linear and circular RNAs. Neurosci Res. 2019 Oct;147:48-57. doi: 10.1016/j.neures.2018.11.005. Epub 2018 Nov 16.
Ref 4 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. doi: 10.1038/s41573-019-0013-8.
Ref 5 Mechanism of inhibition of the GluA2 AMPA receptor channel opening by talampanel and its enantiomer: the stereochemistry of the 4-methyl group on the diazepine ring of 2,3-benzodiazepine derivatives.ACS Chem Neurosci.2013 Apr 17;4(4):635-44.
Ref 6 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 445).