m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02550)
Name
PQR309
Synonyms
Bimiralisib; PQR309; 1225037-39-7; PI3K-IN-2; PQR-309; UNII-6Z3QHB00LB; 6Z3QHB00LB; 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; 5-[bis(morpholin-4-yl)-1,3,5-triazin-2-yl]-4-(trifluoromethyl)pyridin-2-amine; 5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; Bimiralisib [INN]; Bimiralisib [USAN]; PQR309; Bimiralisib; Bimiralisib [WHO-DD]; NCB5; SCHEMBL1309049; GTPL8383; PQR309; Bimiralisib free base; ADGGYDAFIHSYFI-UHFFFAOYSA-N; EX-A2018; BCP15887; PQR-309(PI3K-IN-2)
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Status
Phase 2
Structure
Formula
C17H20F3N7O2
InChI
1S/C17H20F3N7O2/c18-17(19,20)12-9-13(21)22-10-11(12)14-23-15(26-1-5-28-6-2-26)25-16(24-14)27-3-7-29-8-4-27/h9-10H,1-8H2,(H2,21,22)
InChIKey
ADGGYDAFIHSYFI-UHFFFAOYSA-N
PubChem CID
58507717
TTD Drug ID
D0TU7B
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.
PI3-kinase beta (PIK3CB)
Methyltransferase-like 13 (METTL13)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PQR309. The Methyltransferase-like 13 (METTL13) has potential in affecting the response of PQR309 through regulating the expression of PI3-kinase beta (PIK3CB). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PQR309. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of PQR309 through regulating the expression of PI3-kinase beta (PIK3CB). [1], [2]
Wilms tumor 1-associating protein (WTAP)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PQR309. The Wilms tumor 1-associating protein (WTAP) has potential in affecting the response of PQR309 through regulating the expression of PI3-kinase beta (PIK3CB). [1], [2]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PQR309. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of PQR309 through regulating the expression of PI3-kinase beta (PIK3CB). [1], [2]
Serine/threonine-protein kinase mTOR (mTOR)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for PQR309. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of PQR309 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [3]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for PQR309. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of PQR309 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [4]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for PQR309. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PQR309 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [5]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for PQR309. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of PQR309 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [6]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for PQR309. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of PQR309 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [2], [3]
References
Ref 1 N(6)-methyladenosine mRNA methylation of PIK3CB regulates AKT signalling to promote PTEN-deficient pancreatic cancer progression. Gut. 2020 Dec;69(12):2180-2192. doi: 10.1136/gutjnl-2019-320179. Epub 2020 Apr 20.
Ref 2 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44. doi: 10.1038/nrd2926.
Ref 3 Targeting ATF4-dependent pro-survival autophagy to synergize glutaminolysis inhibition. Theranostics. 2021 Jul 25;11(17):8464-8479. doi: 10.7150/thno.60028. eCollection 2021.
Ref 4 The m6A methyltransferase METTL14 inhibits the proliferation, migration, and invasion of gastric cancer by regulating the PI3K/AKT/mTOR signaling pathway. J Clin Lab Anal. 2021 Mar;35(3):e23655. doi: 10.1002/jcla.23655. Epub 2020 Dec 12.
Ref 5 Methyltransferase-like 3 promotes the progression of lung cancer via activating PI3K/AKT/mTOR pathway. Clin Exp Pharmacol Physiol. 2022 Jul;49(7):748-758. doi: 10.1111/1440-1681.13647. Epub 2022 May 23.
Ref 6 YTHDF1 promotes hepatocellular carcinoma progression via activating PI3K/AKT/mTOR signaling pathway and inducing epithelial-mesenchymal transition. Exp Hematol Oncol. 2021 Jun 4;10(1):35. doi: 10.1186/s40164-021-00227-0.