m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02174)
Name
Gilteritinib
Synonyms
UNII-66D92MGC8M; 66D92MGC8M; Gilteritinib [USAN:INN]; Gilteritinib(ASP2215); Gilteritinib (USAN/INN); Gilteritinib (ASP2215); Gilteritinib (ASP-2215); SCHEMBL282229; GTPL8708; MolPort-038-934-933; BDBM144315; C29H44N8O3; 3694AH; s7754; AKOS030234455; ZINC113476229; DB12141; CS-3885; KS-0000064E; AS-35199
    Click to Show/Hide
Status
Approved
Structure
Formula
C29H44N8O3
InChI
1S/C29H44N8O3/c1-4-23-28(31-20-9-17-40-18-10-20)34-29(26(33-23)27(30)38)32-21-5-6-24(25(19-21)39-3)37-11-7-22(8-12-37)36-15-13-35(2)14-16-36/h5-6,19-20,22H,4,7-18H2,1-3H3,(H2,30,38)(H2,31,32,34)
InChIKey
GYQYAJJFPNQOOW-UHFFFAOYSA-N
PubChem CID
49803313
TTD Drug ID
D04KZY
VARIDT Drug ID
DR00358
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.
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 Gilteritinib. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Gilteritinib through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [2]
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 Gilteritinib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Gilteritinib through regulating the expression of P-glycoprotein 1 (ABCB1). [2], [3]
Tyrosine-protein kinase UFO (AXL)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Tyrosine-protein kinase UFO (AXL) is a therapeutic target for Gilteritinib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Gilteritinib through regulating the expression of Tyrosine-protein kinase UFO (AXL). [4], [5]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Tyrosine-protein kinase UFO (AXL) is a therapeutic target for Gilteritinib. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of Gilteritinib through regulating the expression of Tyrosine-protein kinase UFO (AXL). [5], [6]
References
Ref 1 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 2 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01665)
Ref 3 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 4 METTL3 promotes ovarian carcinoma growth and invasion through the regulation of AXL translation and epithelial to mesenchymal transition. Gynecol Oncol. 2018 Nov;151(2):356-365. doi: 10.1016/j.ygyno.2018.09.015. Epub 2018 Sep 21.
Ref 5 Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors. J Med Chem. 2015 Jul 23;58(14):5649-73. doi: 10.1021/acs.jmedchem.5b00772. Epub 2015 Jul 9.
Ref 6 Leukemogenic Chromatin Alterations Promote AML Leukemia Stem Cells via a KDM4C-ALKBH5-AXL Signaling Axis. Cell Stem Cell. 2020 Jul 2;27(1):81-97.e8. doi: 10.1016/j.stem.2020.04.001. Epub 2020 May 12.