m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00520)
Name
APTO-253
Status
Phase 1
Structure
Formula
C22H14FN5
InChI
1S/C22H14FN5/c1-11-17(15-10-12(23)6-7-16(15)26-11)22-27-20-13-4-2-8-24-18(13)19-14(21(20)28-22)5-3-9-25-19/h2-10,26H,1H3,(H,27,28)
InChIKey
NIRXBXIPHUTNNI-UHFFFAOYSA-N
PubChem CID
11960271
TTD Drug ID
D07TRP
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.
Kruppel like factor 4 (KLF4)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Kruppel like factor 4 (KLF4) is a therapeutic target for APTO-253. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of APTO-253 through regulating the expression of Kruppel like factor 4 (KLF4). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Kruppel like factor 4 (KLF4) is a therapeutic target for APTO-253. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of APTO-253 through regulating the expression of Kruppel like factor 4 (KLF4). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Kruppel like factor 4 (KLF4) is a therapeutic target for APTO-253. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of APTO-253 through regulating the expression of Kruppel like factor 4 (KLF4). [2], [4]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Kruppel like factor 4 (KLF4) is a therapeutic target for APTO-253. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of APTO-253 through regulating the expression of Kruppel like factor 4 (KLF4). [2], [3]
References
Ref 1 Methyl CpG binding protein 2 promotes colorectal cancer metastasis by regulating N(6) -methyladenosine methylation through methyltransferase-like 14. Cancer Sci. 2021 Aug;112(8):3243-3254. doi: 10.1111/cas.15011. Epub 2021 Jun 29.
Ref 2 Phase 2 randomized study of p53 antisense oligonucleotide (cenersen) plus idarubicin with or without cytarabine in refractory and relapsed acute myeloid leukemia. Cancer. 2012 Jan 15;118(2):418-27. doi: 10.1002/cncr.26292. Epub 2011 Jun 29.
Ref 3 METTL3/YTHDF2 m(6) A axis promotes tumorigenesis by degrading SETD7 and KLF4 mRNAs in bladder cancer. J Cell Mol Med. 2020 Apr;24(7):4092-4104. doi: 10.1111/jcmm.15063. Epub 2020 Mar 3.
Ref 4 Hypoxia-inducible factors regulate pluripotency factor expression by ZNF217- and ALKBH5-mediated modulation of RNA methylation in breast cancer cells. Oncotarget. 2016 Oct 4;7(40):64527-64542. doi: 10.18632/oncotarget.11743.