m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00099)
Name
Binimetinib
Synonyms
181R97MR71; 5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide; 6-(4-bromo-2-fluorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide; 606143-89-9; ARRY 162; ARRY 438162; ARRY-162; ARRY-438162; Binimetinib (JAN/USAN); Binimetinib (MEK162, ARRY-162, ARRY-438162); Binimetinib [USAN:INN]; D0C4LF; MEK 162; MEK-162; MEK162; MEK162 (ARRY-162, ARRY-438162); MEK162(Binimetinib); NVP-ME; UNII-181R97MR71
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Status
Approved
Structure
Formula
C17H15BrF2N4O3
InChI
1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)
InChIKey
ACWZRVQXLIRSDF-UHFFFAOYSA-N
PubChem CID
10288191
VARIDT Drug ID
DR01336
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 Binimetinib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Binimetinib through regulating the expression of Breast cancer resistance protein (ABCG2). [1], [2]
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 Binimetinib. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Binimetinib through regulating the expression of P-glycoprotein 1 (ABCB1). [2], [3]
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 Binimetinib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Binimetinib through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [2]
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 The impact of P-glycoprotein and breast cancer resistance protein on the brain pharmacokinetics and pharmacodynamics of a panel of MEK inhibitors. Int J Cancer. 2018 Jan 15;142(2):381-391. doi: 10.1002/ijc.31052. Epub 2017 Oct 4.
Ref 3 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.