General Information of the Drug (ID: M6APDG02159)
Name
PA-799
Synonyms
MEN1611; CH-5033855; CH-5061565; CH-5089788; CH-5108135; CH-5111436; CH-5138134
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Status
Phase 1/2
Structure
Formula
C15H19N7O3S
InChI
1S/C15H19N7O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21/h8-9H,2-7H2,1H3,(H2,16,17,18)
InChIKey
JEGHXKRHKHPBJD-UHFFFAOYSA-N
PubChem CID
49784945
TTD Drug ID
D05CBJ
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 alpha (PIK3CA)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase alpha (PIK3CA) is a therapeutic target for PA-799. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase alpha (PIK3CA). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase alpha (PIK3CA) is a therapeutic target for PA-799. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase alpha (PIK3CA). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase alpha (PIK3CA) is a therapeutic target for PA-799. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase alpha (PIK3CA). [2], [4]
PI3-kinase beta (PIK3CB)
Methyltransferase-like 13 (METTL13)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PA-799. The Methyltransferase-like 13 (METTL13) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase beta (PIK3CB). [5], [6]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PA-799. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase beta (PIK3CB). [5], [6]
Wilms tumor 1-associating protein (WTAP)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PA-799. The Wilms tumor 1-associating protein (WTAP) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase beta (PIK3CB). [5], [6]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase beta (PIK3CB) is a therapeutic target for PA-799. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of PA-799 through regulating the expression of PI3-kinase beta (PIK3CB). [5], [6]
References
Ref 1 METTL14 Inhibits Hepatocellular Carcinoma Metastasis Through Regulating EGFR/PI3K/AKT Signaling Pathway in an m6A-Dependent Manner. Cancer Manag Res. 2020 Dec 23;12:13173-13184. doi: 10.2147/CMAR.S286275. eCollection 2020.
Ref 2 ETP-46321, a dual p110Alpha/Delta class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis. Biochem Pharmacol. 2016 Apr 15;106:56-69. doi: 10.1016/j.bcp.2016.02.005. Epub 2016 Feb 13.
Ref 3 Gene signatures and prognostic values of m6A regulators in clear cell renal cell carcinoma - a retrospective study using TCGA database. Aging (Albany NY). 2019 Mar 15;11(6):1633-1647. doi: 10.18632/aging.101856.
Ref 4 ALKBH5 inhibited autophagy of epithelial ovarian cancer through miR-7 and BCL-2. J Exp Clin Cancer Res. 2019 Apr 15;38(1):163. doi: 10.1186/s13046-019-1159-2.
Ref 5 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 6 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401. doi: 10.1021/jm400915j. Epub 2013 Aug 1.