m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02230)
Name
APIGENIN
Synonyms
apigenin; 520-36-5; 5,7-Dihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one; Chamomile; Versulin; Spigenin; Apigenol; 4',5,7-Trihydroxyflavone; Apigenine; C.I. Natural Yellow 1; 5,7,4'-Trihydroxyflavone; Pelargidenon 1449; 5,7-Dihydroxy-2-(4-hydroxyphenyl)-4-benzopyrone; 2-(p-Hydroxyphenyl)-5,7-dihydroxychromone; UCCF 031; NSC 83244; UNII-7V515PI7F6; 5,7-Dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one; 5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one; CCRIS 3789; CHEBI:18388; CHEMBL28; EINECS 208-292-3; 4H-1-Benzopyran-4-one, 5,7-di
    Click to Show/Hide
Status
Investigative
Structure
Formula
C15H10O5
InChI
1S/C15H10O5/c16-9-3-1-8(2-4-9)13-7-12(19)15-11(18)5-10(17)6-14(15)20-13/h1-7,16-18H
InChIKey
KZNIFHPLKGYRTM-UHFFFAOYSA-N
PubChem CID
5280443
TTD Drug ID
D00RIX
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.
Androgen receptor (AR)
ETS-related transcription factor Elf-3 (ELF3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Androgen receptor (AR) is a therapeutic target for APIGENIN. The ETS-related transcription factor Elf-3 (ELF3) has potential in affecting the response of APIGENIN through regulating the expression of Androgen receptor (AR). [1], [2]
Aromatase (CYP19A1)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Aromatase (CYP19A1) is a therapeutic target for APIGENIN. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of APIGENIN through regulating the expression of Aromatase (CYP19A1). [3], [4]
Cyclin-dependent kinase 6 (CDK6)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 6 (CDK6) is a therapeutic target for APIGENIN. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of APIGENIN through regulating the expression of Cyclin-dependent kinase 6 (CDK6). [5], [6]
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 APIGENIN. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of APIGENIN through regulating the expression of Cytochrome P450 1B1 (CYP1B1). [7], [8]
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 APIGENIN. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of APIGENIN through regulating the expression of Cytochrome P450 1B1 (CYP1B1). [8], [9]
References
Ref 1 ELF3 is a repressor of androgen receptor action in prostate cancer cells. Oncogene. 2014 Feb 13;33(7):862-71. doi: 10.1038/onc.2013.15. Epub 2013 Feb 25.
Ref 2 5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. J Med Chem. 1998 Oct 22;41(22):4354-9. doi: 10.1021/jm980366a.
Ref 3 Increased N6-methyladenosine causes infertility is associated with FTO expression. J Cell Physiol. 2018 Sep;233(9):7055-7066. doi: 10.1002/jcp.26507. Epub 2018 Mar 25.
Ref 4 Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. doi: 10.1016/j.bmcl.2010.03.113. Epub 2010 Apr 8.
Ref 5 FTO promotes tumour proliferation in bladder cancer via the FTO/miR-576/CDK6 axis in an m6A-dependent manner. Cell Death Discov. 2021 Nov 1;7(1):329. doi: 10.1038/s41420-021-00724-5.
Ref 6 Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005 Feb 10;48(3):737-43. doi: 10.1021/jm049353p.
Ref 7 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 8 Selective inhibition of methoxyflavonoids on human CYP1B1 activity. Bioorg Med Chem. 2010 Sep 1;18(17):6310-5. doi: 10.1016/j.bmc.2010.07.020. Epub 2010 Jul 13.
Ref 9 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.