m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00335)
Name
ENMD-1198
Synonyms
EM-5171; EM-883; EM-900; Hypoxia inducible factor 1 inhibitors, EntreMed; HIF-1 inhibitors, EntreMed; HIF-1 inhibitors (cancer), EntreMed; 2-ME2 analogs (oral, cancer), EntreMed; 2-methoxyestradiol analogs (oral, cancer), EntreMed
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Status
Phase 1
Structure
Formula
C20H25NO2
InChI
1S/C20H25NO2/c1-20-8-3-4-17(20)14-6-5-12-10-16(19(21)22)18(23-2)11-15(12)13(14)7-9-20/h3,8,10-11,13-14,17H,4-7,9H2,1-2H3,(H2,21,22)/t13-,14+,17-,20-/m0/s1
InChIKey
YQJWOUQGXATDAE-ACNBBOPNSA-N
PubChem CID
11483754
TTD Drug ID
D0Y5QD
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.
Hypoxia-inducible factor 1 alpha (HIF-1A)
Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for ENMD-1198. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of ENMD-1198 through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for ENMD-1198. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of ENMD-1198 through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for ENMD-1198. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of ENMD-1198 through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [2], [4]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Hypoxia-inducible factor 1 alpha (HIF-1A) is a therapeutic target for ENMD-1198. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of ENMD-1198 through regulating the expression of Hypoxia-inducible factor 1 alpha (HIF-1A). [2], [5]
References
Ref 1 Knockdown of m6A Reader IGF2BP3 Inhibited Hypoxia-Induced Cell Migration and Angiogenesis by Regulating Hypoxia Inducible Factor-1Alpha in Stomach Cancer. Front Oncol. 2021 Sep 21;11:711207. doi: 10.3389/fonc.2021.711207. eCollection 2021.
Ref 2 Pilot trial of EZN-2968, an antisense oligonucleotide inhibitor of hypoxia-inducible factor-1 alpha (HIF-1Alpha), in patients with refractory solid tumors. Cancer Chemother Pharmacol. 2014 Feb;73(2):343-8. doi: 10.1007/s00280-013-2362-z. Epub 2013 Nov 30.
Ref 3 HBXIP drives metabolic reprogramming in hepatocellular carcinoma cells via METTL3-mediated m6A modification of HIF-1Alpha. J Cell Physiol. 2021 May;236(5):3863-3880. doi: 10.1002/jcp.30128. Epub 2020 Dec 11.
Ref 4 Hypoxia induces an endometrial cancer stem-like cell phenotype via HIF-dependent demethylation of SOX2 mRNA. Oncogenesis. 2020 Sep 11;9(9):81. doi: 10.1038/s41389-020-00265-z.
Ref 5 RNA helicase YTHDC2 promotes cancer metastasis via the enhancement of the efficiency by which HIF-1Alpha mRNA is translated. Cancer Lett. 2016 Jun 28;376(1):34-42. doi: 10.1016/j.canlet.2016.02.022. Epub 2016 Mar 17.