m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT05362
 [1]
Non-coding RNA RPPH1 IGF2BP2  lncRNA       miRNA   circRNA Direct Enhancement m6A modification FGFR2 FGFR2 IGF2BP2 : m6A sites
m6A Modification:
m6A Regulator Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) READER
 Regulator Info 
m6A Target Fibroblast growth factor receptor 2 (FGFR2)
 Targert Gene 
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Non-coding RNA (ncRNA)
Epigenetic Regulator Ribonuclease P RNA component H1 (RPPH1) 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 Hypoxia induced cellular and exosomal RPPH1 promotes breast cancer angiogenesis and metastasis through stabilizing the IGF2BP2/Fibroblast growth factor receptor 2 (FGFR2) axis
Responsed Disease Breast cancer ICD-11: 2C60
 Disease Info 
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Fibroblast growth factor receptor 2 (FGFR2) 19 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Interferon Alfa-2a, Recombinant Approved [2]
Synonyms
Roferon A (TN)
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MOA Binder
External Link
TTD: D09PMV
 Compound Name Palifermin Approved [3]
Synonyms
Kepivance; Kepivance (TN); Palifermin (USAN/INN)
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MOA Binder
External Link
TTD: D0O7GU
 Compound Name Pemigatinib Approved [4]
Synonyms
Unii-Y6BX7BL23K; Y6BX7BL23K; GTPL9767; SCHEMBL15556271; HCDMJFOHIXMBOV-UHFFFAOYSA-N; example 126 [WO2014007951]; 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one; 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one; INCB54828
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MOA Inhibitor
External Link
CID: 86705695
TTD: D0O6UY
DrugBank: DB15102
 Compound Name Trafermin Phase 3 [5]
Synonyms
Fiblast; Fiblast (TN); Trafermin (genetical recombination); Trafermin (USAN/INN); Trafermin (genetical recombination) (JAN)
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MOA Activator
External Link
TTD: D0KV1Q
 Compound Name E-3810 Phase 3 [6]
Synonyms
Lucitanib; AL-3810; E-3810, EOS
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MOA Inhibitor
Activity IC50 = 82.5 nM
External Link
CID: 25031915
TTD: D02WVT
DrugBank: DB11845
 Compound Name LY2874455 Phase 2 [7]
Synonyms
1254473-64-7; LY-2874455; UNII-E9M363811V; CHEMBL3828009; E9M363811V; AK186860; LY 2874455; (R,E)-2-(4-(2-(5-(1-(3,5-Dichloropyridin-4-yl)-ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol; C21H19Cl2N5O2; (R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol; GKJCVYLDJWTWQU-CXLRFSCWSA-N; SCHEMBL298446; SCHEMBL298445; QCR-90; GTPL8104; DTXSID20154776; MolPort-044-724-281; MolPort-023-219-117; EX-A1340; BCP04756; ZINC73069242; BDBM50189781; 2529AH; s7057; AKOS027251051
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MOA Modulator
Activity IC50 = 2.6 nM
External Link
CID: 46944259
TTD: D0D4VV
DrugBank: DB13022
 Compound Name Debio 1347 Phase 2 [8]
MOA Inhibitor
Activity IC50 = 7.6 nM
External Link
CID: 66555680
TTD: D0XT0W
DrugBank: DB12903
 Compound Name AEE-788 Phase 1/2 [9]
Synonyms
AEE; AEE 788; AEE788; GNF-Pf-5343; AEE-788, NVP-AEE 788, AEE788
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MOA Inhibitor
External Link
CID: 10297043
TTD: D0G2QH
DrugBank: DB12558
 Compound Name MK-2461 Phase 1/2 [10]
Synonyms
MK 2461
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MOA Inhibitor
Activity IC50 = 39 nM
External Link
CID: 44137946
TTD: D00DRL
 Compound Name BAY1179470 Phase 1 [11]
MOA Antagonist
External Link
TTD: D0L6RF
 Compound Name Alofanib Phase 1 [12]
Synonyms
1612888-66-0; 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid; RPT-835(alofanib); UNII-LQX7RFK8MZ; RPT-835; RPT835; LQX7RFK8MZ; ES000835; Alofanib [INN]; Alofanib(RPT835); Syn007154; CHEMBL4594436; SCHEMBL18660613; AMY16650; BCP31905; EX-A2731; MFCD30533418; NSC790182; s8754; Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-; NSC-790182; SB19665; AC-31695; AK668992; AS-56846; HY-17601; CS-0014684; RPT 835; Q27283135; 3-{[4-methyl-2-nitro-5-(pyridin-3-yl)phenyl]sulfamoyl}benzoic acid
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MOA Inhibitor
External Link
CID: 86280646
TTD: D47MOS
 Compound Name RLY-4008 Phase 1 [13]
MOA Inhibitor
External Link
TTD: DU1DL0
 Compound Name PD-0183812 Terminated [14]
Synonyms
PETCVZZPKYJZAU-UHFFFAOYSA-N; PD183812; AC1NS8PJ; CHEMBL139653; SCHEMBL5268115; BDBM6280; PD 0183812; N8 Pyrido[2,3-d]pyrimidin-7-one deriv 72; 8-{bicyclo[221]heptan-2-yl}-2-({4-[4-(3-hydroxypropyl)piperidin-1-yl]phenyl}amino)-7H,8H-pyrido[2,3-d]pyrimidin-7-one; 8-(3-bicyclo[221]heptanyl)-2-[4-[4-(3-hydroxypropyl)piperidin-1-yl]anilino]pyrido[2,3-d]pyrimidin-7-one; PD0183813
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MOA Inhibitor
External Link
CID: 5330258
TTD: D0Z0KD
 Compound Name Anti-FGFR2 humanized mab Investigative [15]
Synonyms
HuGAL-FR21; HuGAL-FR22; Anti-FGFR2 humanized mAb (cancer); Anti-FGFR2 humanized mAb (cancer), Galaxy
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External Link
TTD: D02VPS
 Compound Name Platelet factor 4 (PF-4) Investigative [16]
Synonyms
Platelet factor 4 (59-70); 88145-47-5; PF4 (59-70); DTXSID30236855; L-Serine, N-(N-(N-(N-(N2-(N2-(N-(N-(N2-(N2-(N-L-leucyl-L-tyrosyl)-L-lysyl)-L-lysyl)-L-isoleucyl)-L-isoleucyl)-L-lysyl)-L-lysyl)-L-leucyl)-L-leucyl)-L-alpha-glutamyl)-, (6R-(6alpha,7beta(Z)))-
    Click to Show/Hide
MOA Inhibitor
External Link
CID: 56842294
TTD: D0IE6Z
 Compound Name PK 11195 Investigative [2]
Synonyms
1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide; 85532-75-8; PK-11195; PK11195; RP 52028; BRN 4264456; CHEBI:73290; N-sec-butyl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide; N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide; N-(butan-2-yl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide; 3-Isoquinolinecarboxamide, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-; SMR000058427; SR-01000076240; Biomol-NT_000287; AC1L1B9T; DSSTox_RID_79625; Interferon alfa (IFN-alpha)
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MOA Binder
External Link
CID: 1345
TTD: D0VN4K
 Compound Name ACTB-1003 Investigative [15]
Synonyms
Multi-mode kinase inhibitor (oral, cancer), ACT Biotech; Multi-mode kinase inhibitor (oral, cancer), Bayer
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MOA Inhibitor
External Link
CID: 23653175
TTD: D0R6OM
 Compound Name TG-100435 Investigative [17]
Synonyms
CHEMBL230686; SCHEMBL4266197; ZINC28702706; BDBM50198782; US8481536, 367; US8481536, 575; ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine); 7-(2,6-dichlorophenyl)-5-methyl-N-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)benzo[e][1,2,4]triazin-3-amine
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MOA Inhibitor
Activity Ki = 493 nM
External Link
CID: 11562302
TTD: D0H1OK
 Compound Name Ro-4396686 Investigative [18]
Synonyms
SCHEMBL5809947; CHEMBL606964
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MOA Inhibitor
External Link
CID: 11396738
TTD: D09XIL
2C60: Breast cancer 2 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Entrectinib Approved [19]
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 [20]
External Link
CID: 6442177
TTD: D09ZSC
DrugBank: DB01590
References
Ref 1 Hypoxia induced cellular and exosomal RPPH1 promotes breast cancer angiogenesis and metastasis through stabilizing the IGF2BP2/FGFR2 axis. Oncogene. 2025 Feb;44(3):147-164. doi: 10.1038/s41388-024-03213-y. Epub 2024 Nov 4.
Ref 2 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. doi: 10.1093/nar/gkm958. Epub 2007 Nov 29.
Ref 3 Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
Ref 4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
Ref 5 Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. doi: 10.1517/14728214.11.4.709.
Ref 6 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6.
Ref 7 Company report (Eli Lilly) (drug: LY2874455)
Ref 8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 9 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 10 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9.
Ref 11 National Cancer Institute Drug Dictionary (drug id 751593).
Ref 12 Corrigendum to 'Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models' [Eur J Cancer 61 (2016) 20-28]. Eur J Cancer. 2017 Jan;70:156.
Ref 13 Clinical pipeline report, company report or official report of Relay Therapeutics.
Ref 14 Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16. doi: 10.1021/jm000271k.
Ref 15 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: 1809).
Ref 16 A short peptide domain of platelet factor 4 blocks angiogenic key events induced by FGF-2. FASEB J. 2001 Mar;15(3):550-2.
Ref 17 Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. doi: 10.1016/j.bmcl.2006.11.006. Epub 2006 Nov 7.
Ref 18 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. doi: 10.1016/j.bmcl.2005.12.092. Epub 2006 Feb 3.
Ref 19 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 20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015