m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG03345)
Name
Estradiol
Synonyms
Aerodiol; Altrad; Aquadiol; Bardiol; Climara; Corpagen; Dihydrofolliculin; Dihydromenformon; Dihydrotheelin; Dihydroxyestrin; Dimenformon; Diogyn; Diogynets; Divigel; Estrace; Estraderm TTS; Estroclim; Estrovite; Evorel; Femestral; Femogen; Follicyclin; Ginosedol; Gynergon; Gynoestryl; Lamdiol; Macrodiol; Oestergon; Oestradiol; Oestroglandol; Ovahormon; Ovasterol; Ovastevol; Ovocyclin; Perlatanol; Primofol; Profoliol; Syndiol; Trocosone; Vagifem; Vivelle; beta-Estradiol; cis-Estradiol; estradiol; estradiol-17beta; progynon; 17beta-Estradiol; 50-28-2
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Status
Approved
Structure
Formula
C18H24O2
InChI
1S/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1
InChIKey
VOXZDWNPVJITMN-ZBRFXRBCSA-N
PubChem CID
5757
VARIDT Drug ID
DR00129
INTEDE Drug ID
DR0007
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.
Breast cancer resistance protein (ABCG2)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Breast cancer resistance protein (ABCG2) is a therapeutic target for Estradiol. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Estradiol through regulating the expression of Breast cancer resistance protein (ABCG2). [1], [2]
Cytochrome P450 1B1 (CYP1B1)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 1B1 (CYP1B1) is a therapeutic target for Estradiol. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Estradiol through regulating the expression of Cytochrome P450 1B1 (CYP1B1). [3], [4]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 1B1 (CYP1B1) is a therapeutic target for Estradiol. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Estradiol through regulating the expression of Cytochrome P450 1B1 (CYP1B1). [4], [5]
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Estradiol. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Estradiol through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [6], [7]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Estradiol. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Estradiol through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [6], [7]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Estradiol. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Estradiol through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [6], [7]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Estradiol. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Estradiol through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [6], [7]
P-glycoprotein 1 (ABCB1)
Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Estradiol. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Estradiol through regulating the expression of P-glycoprotein 1 (ABCB1). [8], [9]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Estradiol. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Estradiol through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [9]
References
Ref 1 METTL3 promotes adriamycin resistance in MCF-7 breast cancer cells by accelerating pri-microRNA-221-3p maturation in a m6A-dependent manner. Exp Mol Med. 2021 Jan;53(1):91-102. doi: 10.1038/s12276-020-00510-w. Epub 2021 Jan 8.
Ref 2 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51. doi: 10.1074/jbc.M301358200. Epub 2003 Mar 28.
Ref 3 LNC942 promoting METTL14-mediated m(6)A methylation in breast cancer cell proliferation and progression. Oncogene. 2020 Jul;39(31):5358-5372. doi: 10.1038/s41388-020-1338-9. Epub 2020 Jun 23.
Ref 4 Cytochrome P450 isoforms catalyze formation of catechol estrogen quinones that react with DNA. Metabolism. 2007 Jul;56(7):887-94. doi: 10.1016/j.metabol.2007.03.001.
Ref 5 METTL3 contributes to renal ischemia-reperfusion injury by regulating Foxd1 methylation. Am J Physiol Renal Physiol. 2020 Nov 1;319(5):F839-F847. doi: 10.1152/ajprenal.00222.2020. Epub 2020 Sep 21.
Ref 6 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 7 Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411.
Ref 8 Binding of RNA m6A by IGF2BP3 triggers chemoresistance of HCT8 cells via upregulation of ABCB1. Am J Cancer Res. 2021 Apr 15;11(4):1428-1445. eCollection 2021.
Ref 9 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. doi: 10.1016/0006-2952(94)90099-x.