m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00284)
Name
Riociguat
Synonyms
Riociguat; Riociguat (BAY 63-2521); riociguatum; 625115-55-1; BAY 63-2521; BAY 632521; CHEBI:76018; Adempas; RU3FE2Y4XI; Methyl (4,6-diamino-2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-5-yl)(methyl)carbamate; Methyl N-(4,6-diamino-2-{1-((2-fluorophenyl)methyl)-1H-pyrazolo(3,4-b)pyridin-3-yl}pyrimidin-5-yl)-N-methylcarbamate; N-[4,6-Diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methylcarbamic acid methyl ester; UNII-RU3FE2Y4XI
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Status
Approved
Structure
Formula
C20H19FN8O2
InChI
1S/C20H19FN8O2/c1-28(20(30)31-2)15-16(22)25-18(26-17(15)23)14-12-7-5-9-24-19(12)29(27-14)10-11-6-3-4-8-13(11)21/h3-9H,10H2,1-2H3,(H4,22,23,25,26)
InChIKey
WXXSNCNJFUAIDG-UHFFFAOYSA-N
PubChem CID
11304743
VARIDT Drug ID
DR00080
INTEDE Drug ID
DR1427
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 Riociguat. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Riociguat through regulating the expression of Breast cancer resistance protein (ABCG2). [1], [2]
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 Riociguat. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Riociguat through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Riociguat. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Riociguat through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Riociguat. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Riociguat through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Riociguat. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Riociguat through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Riociguat. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Riociguat through regulating the expression of P-glycoprotein 1 (ABCB1). [5], [6]
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 Riociguat. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Riociguat through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [6]
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 KEGG: new perspectives on genomes, pathways, diseases and drugs. Nucleic Acids Res. 2017 Jan 4;45(D1):D353-D361. (dg:DG01913)
Ref 3 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 4 Riociguat (adempas): a novel agent for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. P T. 2014 Nov;39(11):749-58.
Ref 5 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 6 Pharmacokinetic interaction profile of riociguat, a new soluble guanylate cyclase stimulator, in?vitro. Pulm Pharmacol Ther. 2014 Aug;28(2):130-7. doi: 10.1016/j.pupt.2014.02.004. Epub 2014 Mar 21.