General Information of the Drug (ID: M6APDG03230)
Name
PKF-242-484
Synonyms
TNF-484
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Status
Investigative
Structure
Formula
C19H29N3O6
InChI
1S/C19H29N3O6/c1-19(2,3)15(18(26)20-4)21-17(25)14(13(10-23)16(24)22-27)11-6-8-12(28-5)9-7-11/h6-9,13-15,23,27H,10H2,1-5H3,(H,20,26)(H,21,25)(H,22,24)/t13-,14+,15+/m0/s1
InChIKey
IOLRUMINDIUCLJ-RRFJBIMHSA-N
PubChem CID
9886977
TTD Drug ID
D0H2PA
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.
Matrix metalloproteinase-1 (MMP-1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-1 (MMP-1) is a therapeutic target for PKF-242-484. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PKF-242-484 through regulating the expression of Matrix metalloproteinase-1 (MMP-1). [1], [2]
Matrix metalloproteinase-13 (MMP-13)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-13 (MMP-13) is a therapeutic target for PKF-242-484. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of PKF-242-484 through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [2], [3]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-13 (MMP-13) is a therapeutic target for PKF-242-484. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PKF-242-484 through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [2], [4]
Matrix metalloproteinase-3 (MMP-3)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-3 (MMP-3) is a therapeutic target for PKF-242-484. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PKF-242-484 through regulating the expression of Matrix metalloproteinase-3 (MMP-3). [5], [6]
Tumor necrosis factor (TNF)
Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)
In total 1 mechanisms lead to this potential drug response
Response Summary Tumor necrosis factor (TNF) is a therapeutic target for PKF-242-484. The Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) has potential in affecting the response of PKF-242-484 through regulating the expression of Tumor necrosis factor (TNF). [7], [8]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Tumor necrosis factor (TNF) is a therapeutic target for PKF-242-484. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of PKF-242-484 through regulating the expression of Tumor necrosis factor (TNF). [8], [9]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Tumor necrosis factor (TNF) is a therapeutic target for PKF-242-484. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PKF-242-484 through regulating the expression of Tumor necrosis factor (TNF). [8], [10]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary Tumor necrosis factor (TNF) is a therapeutic target for PKF-242-484. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of PKF-242-484 through regulating the expression of Tumor necrosis factor (TNF). [8], [10]
YTH domain-containing family protein 3 (YTHDF3)
In total 1 mechanisms lead to this potential drug response
Response Summary Tumor necrosis factor (TNF) is a therapeutic target for PKF-242-484. The YTH domain-containing family protein 3 (YTHDF3) has potential in affecting the response of PKF-242-484 through regulating the expression of Tumor necrosis factor (TNF). [7], [8]
References
Ref 1 METTL3 involves the progression of osteoarthritis probably by affecting ECM degradation and regulating the inflammatory response. Life Sci. 2021 Aug 1;278:119528. doi: 10.1016/j.lfs.2021.119528. Epub 2021 Apr 21.
Ref 2 Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. doi: 10.1016/j.bmcl.2006.01.055. Epub 2006 Feb 10.
Ref 3 FTO promotes cell proliferation and migration in esophageal squamous cell carcinoma through up-regulation of MMP13. Exp Cell Res. 2020 Apr 1;389(1):111894. doi: 10.1016/j.yexcr.2020.111894. Epub 2020 Feb 6.
Ref 4 METTL3 promotes experimental osteoarthritis development by regulating inflammatory response and apoptosis in chondrocyte. Biochem Biophys Res Commun. 2019 Aug 13;516(1):22-27. doi: 10.1016/j.bbrc.2019.05.168. Epub 2019 Jun 8.
Ref 5 METTL3 Promotes Activation and Inflammation of FLSs Through the NF-KappaB Signaling Pathway in Rheumatoid Arthritis. Front Med (Lausanne). 2021 Jul 6;8:607585. doi: 10.3389/fmed.2021.607585. eCollection 2021.
Ref 6 Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates. J Med Chem. 2006 Feb 9;49(3):923-31. doi: 10.1021/jm050787+.
Ref 7 N6-methyladenosine reader YTH N6-methyladenosine RNA binding protein 3 or insulin like growth factor 2 mRNA binding protein 2 knockdown protects human bronchial epithelial cells from hypoxia/reoxygenation injury by inactivating p38 MAPK, AKT, ERK1/2, and NF-KappaB pathways. Bioengineered. 2022 May;13(5):11973-11986. doi: 10.1080/21655979.2021.1999550.
Ref 8 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
Ref 9 METTL14 promotes glomerular endothelial cell injury and diabetic nephropathy via m6A modification of Alpha-klotho. Mol Med. 2021 Sep 9;27(1):106. doi: 10.1186/s10020-021-00365-5.
Ref 10 Mettl3 inhibits the apoptosis and autophagy of chondrocytes in inflammation through mediating Bcl2 stability via Ythdf1-mediated m(6)A modification. Bone. 2022 Jan;154:116182. doi: 10.1016/j.bone.2021.116182. Epub 2021 Sep 13.