General Information of the Drug (ID: M6APDG00323)
Name
Apratastat
Synonyms
TMI-005; TMI-05; UNII-C6BZ5263BJ; 287405-51-0; C6BZ5263BJ; CHEMBL206815; TMI 005; Apratastat [USAN:INN]; Apratastat (USAN/INN); MLS006010301; SCHEMBL2834310; GTPL6482; TMI005; Apratastat, > MolPort-021-805-014; BCPP000041; ZINC28571311; BDBM50181008; DB13020; API0013699; compound 5h [PMID: 16426848]; SMR004701369; 4CA-0170; D08859; 3-Thiomorpholinecarboxamide,N-hydroxy-4-[[4-[(4-hydroxy-2-butyn-1-yl)oxy]phenyl]sulfonyl]-2,2-dimethyl-,(3S)-; TMI-1; Dual TACE/MMP-13 inhibitors (inflammation), Wyeth; Dual TACE/MMP-13 inhibitors (rheumatoid arthritis), Wyeth; Dual TACE/MMP-13 inhibitors, Wyeth-Ayerst
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Status
Phase 2
Structure
Formula
C17H22N2O6S2
InChI
1S/C17H22N2O6S2/c1-17(2)15(16(21)18-22)19(9-12-26-17)27(23,24)14-7-5-13(6-8-14)25-11-4-3-10-20/h5-8,15,20,22H,9-12H2,1-2H3,(H,18,21)/t15-/m0/s1
InChIKey
MAVDNGWEBZTACC-HNNXBMFYSA-N
PubChem CID
11452716
TTD Drug ID
D0HG5M
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 Apratastat. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Apratastat 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 Apratastat. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Apratastat through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [3], [4]
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 Apratastat. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Apratastat through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [4], [5]
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 Matrix metalloproteinase inhibition lowers mortality and brain injury in experimental pneumococcal meningitis. Infect Immun. 2014 Apr;82(4):1710-8. doi: 10.1128/IAI.00073-14. Epub 2014 Feb 3.
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 High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate. Bioorg Med Chem. 2009 Feb 1;17(3):990-1005. doi: 10.1016/j.bmc.2008.03.004. Epub 2008 Mar 6.
Ref 5 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.