General Information of the Drug (ID: M6APDG02789)
Name
2-Methoxyestradiol
Synonyms
ESM; Panzem; PulmoLAR; Panzem NCD; M 6383; (17beta)-2-Methoxyestra-1,3,5(10)-triene-3,17-diol; (17beta)-2-methoxyestra-1(10),2,4-triene-3,17-diol; (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; 1,3,5(10)-ESTRATRIEN-2,3,17-BETA-TRIOL 2-METHYL ETHER; 1,3,5(10)-Estratriene-2,3,17-triol 2-methyl ether; 2,3,17beta-Trihydroxy-1,3,5(10)-estratriene 2-methyl ether; 2-Hydroxyestradiol 2-methyl ether; 2-Hydroxyestradol 2-methyl ether; 2-ME2, 2-Methoxyestradiol; 2-Methoxyestra-1,3,5(10)-triene-3,17beta-diol; 2-Methoxyestradiol-17beta; 3,17beta-Dihydroxy-2-methoxy-1,3,5(10)-estratriene
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Status
Phase 2
Structure
Formula
C19H26O3
InChI
1S/C19H26O3/c1-19-8-7-12-13(15(19)5-6-18(19)21)4-3-11-9-16(20)17(22-2)10-14(11)12/h9-10,12-13,15,18,20-21H,3-8H2,1-2H3/t12-,13+,15-,18-,19-/m0/s1
InChIKey
CQOQDQWUFQDJMK-SSTWWWIQSA-N
PubChem CID
66414
TTD Drug ID
D06NYA
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Hypoxia-inducible factor 1 alpha (HIF-1A)
Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3)
In total 1 mechanisms lead to this potential drug response
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for 2-Methoxyestradiol. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of 2-Methoxyestradiol through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for 2-Methoxyestradiol. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of 2-Methoxyestradiol through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for 2-Methoxyestradiol. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of 2-Methoxyestradiol through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [2], [4]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for 2-Methoxyestradiol. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of 2-Methoxyestradiol through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [2], [5]
References
Ref 1 Knockdown of m6A Reader IGF2BP3 Inhibited Hypoxia-Induced Cell Migration and Angiogenesis by Regulating Hypoxia Inducible Factor-1Alpha in Stomach Cancer. Front Oncol. 2021 Sep 21;11:711207. doi: 10.3389/fonc.2021.711207. eCollection 2021.
Ref 2 CRLX101, an investigational camptothecin-containing nanoparticle-drug conjugate, targets cancer stem cells and impedes resistance to antiangiogenic therapy in mouse models of breast cancer. Breast Cancer Res Treat. 2015 Apr;150(3):559-67. doi: 10.1007/s10549-015-3349-8. Epub 2015 Apr 2.
Ref 3 HBXIP drives metabolic reprogramming in hepatocellular carcinoma cells via METTL3-mediated m6A modification of HIF-1Alpha. J Cell Physiol. 2021 May;236(5):3863-3880. doi: 10.1002/jcp.30128. Epub 2020 Dec 11.
Ref 4 Hypoxia induces an endometrial cancer stem-like cell phenotype via HIF-dependent demethylation of SOX2 mRNA. Oncogenesis. 2020 Sep 11;9(9):81. doi: 10.1038/s41389-020-00265-z.
Ref 5 RNA helicase YTHDC2 promotes cancer metastasis via the enhancement of the efficiency by which HIF-1Alpha mRNA is translated. Cancer Lett. 2016 Jun 28;376(1):34-42. doi: 10.1016/j.canlet.2016.02.022. Epub 2016 Mar 17.