General Information of the Drug (ID: M6APDG03828)
Name
ARQ-171
Synonyms
ARQ-550RP; ARQ-580; E2F modulators (anticancer); E2F modulators (anticancer), ArQule; 550 series (E2F modulators), Arqule; 550 series (anticancer), Arqule; 550 series, Arqule
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Status
Phase 1
TTD Drug ID
D00SIA
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.
E2F transcription factor 1 (E2F1)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary E2F transcription factor 1 (E2F1) is a therapeutic target for ARQ-171. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of ARQ-171 through regulating the expression of E2F transcription factor 1 (E2F1). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary E2F transcription factor 1 (E2F1) is a therapeutic target for ARQ-171. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of ARQ-171 through regulating the expression of E2F transcription factor 1 (E2F1). [2], [3]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary E2F transcription factor 1 (E2F1) is a therapeutic target for ARQ-171. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of ARQ-171 through regulating the expression of E2F transcription factor 1 (E2F1). [1], [2]
References
Ref 1 Correlation of m6A methylation with immune infiltrates and poor prognosis in non-small cell lung cancer via a comprehensive analysis of RNA expression profiles. Ann Transl Med. 2021 Sep;9(18):1465. doi: 10.21037/atm-21-4248.
Ref 2 Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J Med Chem. 2009 Oct 22;52(20):6433-46. doi: 10.1021/jm9009444.
Ref 3 Effect of m6A methyltransferase METTL3 -mediated MALAT1/E2F1/AGR2 axis on adriamycin resistance in breast cancer. J Biochem Mol Toxicol. 2022 Jan;36(1):e22922. doi: 10.1002/jbt.22922. Epub 2021 Dec 28.