m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT05307
 [1]
Non-coding RNA A1BG-AS1 IGF2BP2  lncRNA       miRNA   circRNA Direct Enhancement m6A modification ABCB1 ABCB1 IGF2BP2 : m6A sites
m6A Modification:
m6A Regulator Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) READER
 Regulator Info 
m6A Target ATP-dependent translocase ABCB1 (ABCB1)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Non-coding RNA (ncRNA)
Epigenetic Regulator A1BG antisense RNA 1 (A1BG-AS1) LncRNA View Details
Regulated Target Insulin like growth factor 2 mRNA binding protein 2 (IGF2BP2) View Details
Crosstalk Relationship ncRNA  →  m6A Enhancement
Crosstalk Mechanism ncRNAs directly impacts m6A modification through recruiting m6A regulator
Crosstalk Summary A1BG-AS1 promotes adriamycin resistance of breast cancer by recruiting IGF2BP2 to upregulate ATP-dependent translocase ABCB1 (ABCB1) in an m6A-dependent manner
Responsed Disease Breast cancer ICD-11: 2C60
 Disease Info 
Responsed Drug Adriamycin
 Drug Info 
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
ATP-dependent translocase ABCB1 (ABCB1) 18 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name EDP-322 Phase 1 [2]
Synonyms
EP-16322; Antibacterial (oral, Gram-positive infections), Enanta; EDP-MRSA-1 (oral), Enanta
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MOA Inhibitor
External Link
TTD: D09LSY
 Compound Name W-198 Phase 1 [3]
Synonyms
5-Bromotetrandrine
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MOA Modulator
External Link
CID: 9831563
TTD: D0GS2W
 Compound Name CBT-1 Application submitted [4]
MOA Modulator
External Link
TTD: D06XVF
 Compound Name LY335979 Discontinued in Phase 3 [5]
Synonyms
Zosuquidar HCl; Zosuquidar Trihydrochloride; LY 335979; LY-335979; Zosuquidar (TN); Zosuquidar trihydrochloride (USAN); RS-33295-198; Zosuquidar trihydrochloride, RS-33295-198, LY335979; (R)-4-((1aR,6R,10bS)-1,2-Difluoro-1,1a,6,10b-tetrahydrodibenzo(a,e)cyclopropa(c)cycloheptan-6-yl)-alpha-((5-quinoloyloxy)methyl)-1-piperazineethanol, trihydrochloride
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MOA Modulator
Activity IC50 = 3490 nM
External Link
CID: 153997
TTD: D06DCL
 Compound Name Biricodar Discontinued in Phase 2 [6]
Synonyms
Incel; Biricodar [INN]; Vx 710; Incel (TN); 1,7-dipyridin-3-ylheptan-4-yl (2S)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
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MOA Modulator
External Link
CID: 3037617
TTD: D02VJY
DrugBank: DB04851
 Compound Name Tariquidar Discontinued in Phase 2 [7]
Synonyms
Tariquidarth; XR 9576; XR9576; Tariquidar (USAN/INN); N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide; N-(2-((4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)phenyl)carbamoyl)-4,5-dimethoxyphenyl)quinoline-3-carboxamide
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MOA Modulator
Activity IC50 = 0.66 nM
External Link
CID: 148201
TTD: D04RLX
DrugBank: DB06240
 Compound Name S-9788 Discontinued in Phase 2 [8]
Synonyms
S9788; S 9788; CHEMBL85156; 140945-01-3; 6-(4-(2,2-di(4-Fluorophenyl)ethylamino)-1-piperidinyl)-N,N'-di-2-propenyl-1,3,5-triazine-2,4-diamine; 1,3,5-Triazine-2,4-diamine, 6-(4-((2,2-bis(4-fluorophenyl)ethyl)amino)-1-piperidinyl)-N,N'-di-2-propenyl-; AC1L32YH; SCHEMBL1527824; DTXSID80161502; GERNFWKTMKWULM-UHFFFAOYSA-N; BDBM50053888; LS-187603; LS-186957; N,N''-Diallyl-6-{4-[2,2-bis-(4-fluoro-phenyl)-ethylamino]-piperidin-1-yl}-[1,3,5]triazine-2,4-diamine; H2O
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MOA Modulator
External Link
CID: 107903
TTD: D0CO2M
 Compound Name XR-9051 Discontinued in Phase 1 [9]
Synonyms
Multidrug resistance inhibitor, Xenova
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MOA Inhibitor
External Link
CID: 9917447
TTD: D01GDH
 Compound Name Elacridar Discontinued in Phase 1 [10]
Synonyms
Elacridar hydrochloride; 143851-98-3; Elacridar HCl; Elacridar (hydrochloride); gf 120918a; UNII-NX2BHH1A5B; NX2BHH1A5B; Elacridar hydrochloride [USAN]; GF-120918A; Elacridar hydrochloride (USAN); GF 120918; AC1Q3EOG; AC1L55DX; C34H34ClN3O5; SCHEMBL15847793; CHEMBL2074730; AOB5938; MolPort-023-332-877; BCP14056; 7066AA; AKOS016005297; CS-1113; ACN-041487; 4CA-0489; HY-50880; AC-30266; FT-0696337; W-5457; D03968; N-[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]-9,10-dihydro-5-methoxy-9-oxo-4-acridinecarboxamide hydro
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MOA Inhibitor
Activity EC50 = 2000 nM
External Link
CID: 119373
TTD: D09FGX
DrugBank: DB04881
 Compound Name ONT-093 Discontinued in Phase 1 [11]
Synonyms
MDR inhibitors, Ontogen; OC-144-093
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MOA Inhibitor
Activity IC50 = 31.62 nM
External Link
CID: 6450807
TTD: D0SR4G
DrugBank: DB14069
 Compound Name 6-(3,5-dimethoxy-phenyl)-naphthalen-2-ol Investigative [12]
Synonyms
CHEMBL362997; BDBM50186758
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MOA Inhibitor
Activity IC50 = 16000 nM
External Link
CID: 11536458
TTD: D05XGZ
 Compound Name [1,1':2',1'']-terphenyl-4,3'',5''-triol Investigative [12]
Synonyms
CHEMBL208098; BDBM50186757; ZINC35856323
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MOA Inhibitor
Activity IC50 = 12000 nM
External Link
CID: 11579996
TTD: D03PLP
 Compound Name XR-9456 Investigative [13]
Synonyms
CHEMBL346292; SCHEMBL7170174; BDBM50375810
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MOA Inhibitor
Activity IC50 = 251.19 nM
External Link
CID: 15511439
TTD: D04GYT
 Compound Name XR-9504 Investigative [13]
Synonyms
CHEMBL258896; SCHEMBL7168501
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MOA Inhibitor
Activity IC50 = 524.81 nM
External Link
CID: 22004473
TTD: D09HIM
 Compound Name XR-9544 Investigative [13]
Synonyms
CHEMBL444075; SCHEMBL14290581; BDBM50375811
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MOA Inhibitor
Activity IC50 = 165.96 nM
External Link
CID: 15511440
TTD: D0A4TF
 Compound Name 4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl Investigative [12]
Synonyms
CHEMBL379687; BDBM50186763
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MOA Inhibitor
Activity IC50 = 16000 nM
External Link
CID: 11537051
TTD: D0AW4W
 Compound Name XR-9577 Investigative [13]
Synonyms
CHEMBL428402
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MOA Inhibitor
Activity IC50 = 354.81 nM
External Link
CID: 15950351
TTD: D0S8CE
 Compound Name TRISMETHOXYRESVERATROL Investigative [12]
Synonyms
22255-22-7; trans-Trimethoxyresveratrol; (E)-1,3-Dimethoxy-5-(4-methoxystyryl)benzene; (E)-3,5,4'-Trimethoxystilbene; 3,4',5-trimethoxy-trans-stilbene; 3,4',5-trimethoxystilbene; 3,5,4'-trimethoxystilbene; TRIMETHOXYSTILBENE; E-Resveratrol trimethyl ether; CHEMBL296411; 1,3-dimethoxy-5-[(E)-2-(4-methoxyphenyl)ethenyl]benzene; trans-3,4',5-trimethoxystilbene; GDHNBPHYVRHYCC-SNAWJCMRSA-N; (E)-3,4',5-Trimethoxystilbene; 5-[2-(4-Methoxyphenyl)Ethenyl]-1,3-Dimethoxy Benzene
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MOA Inhibitor
Activity IC50 = 8000 nM
External Link
CID: 5388063
TTD: D0O9NE
2C60: Breast cancer 2 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Entrectinib Approved [14]
Synonyms
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
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External Link
CID: 25141092
TTD: D0O0LS
DrugBank: DB11986
 Compound Name Everolimus Approved [15]
External Link
CID: 6442177
TTD: D09ZSC
DrugBank: DB01590
References
Ref 1 A1BG-AS1 promotes adriamycin resistance of breast cancer by recruiting IGF2BP2 to upregulate ABCB1 in an m6A-dependent manner. Sci Rep. 2023 Nov 25;13(1):20730. doi: 10.1038/s41598-023-47956-2.
Ref 2 In vitro activities of the novel bicyclolides modithromycin (EDP-420, EP-013420, S-013420) and EDP-322 against MDR clinical Neisseria gonorrhoeae isolates and international reference strains. J Antimicrob Chemother. 2015 Jan;70(1):173-7. doi: 10.1093/jac/dku344. Epub 2014 Sep 1.
Ref 3 Mechanisms of tetrandrine and 5-bromotetrandrine in reversing multidrug resistance may relate to down-regulation of multidrug resistance associated protein 7 expression. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):558-63.
Ref 4 A pharmacodynamic study of the P-glycoprotein antagonist CBT-1? in combination with paclitaxel in solid tumors. Oncologist. 2012;17(4):512. doi: 10.1634/theoncologist.2012-0080. Epub 2012 Mar 13.
Ref 5 A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxorubicin in patients with advanced malignancy. Clin Cancer Res. 2004 May 15;10(10):3265-72. doi: 10.1158/1078-0432.CCR-03-0644.
Ref 6 ClinicalTrials.gov (NCT00003847) VX-710, Doxorubicin, and Vincristine for the Treatment of Patients With Recurrent Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 7 Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)). Biochem Pharmacol. 2008 Mar 15;75(6):1302-12. doi: 10.1016/j.bcp.2007.12.001. Epub 2007 Dec 14.
Ref 8 In vitro activity of S 9788 on a multidrug-resistant leukemic cell line and on normal hematopoietic cells-reversal of multidrug resistance by sera from phase I-treated patients. Cancer Chemother Pharmacol. 1995;36(3):195-203.
Ref 9 Communication between multiple drug binding sites on P-glycoprotein. Mol Pharmacol. 2000 Sep;58(3):624-32.
Ref 10 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. J Med Chem. 2008 Dec 11;51(23):7602-13. doi: 10.1021/jm800928j.
Ref 11 A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5. doi: 10.1007/s10637-005-1439-x.
Ref 12 Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. J Med Chem. 2006 May 18;49(10):3012-8. doi: 10.1021/jm060253o.
Ref 13 Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. Bioorg Med Chem. 2008 Mar 1;16(5):2448-62. doi: 10.1016/j.bmc.2007.11.057. Epub 2007 Nov 28.
Ref 14 Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372... Cancer Discov. 2017 Apr;7(4):400-409.
Ref 15 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015