General Information of the Drug (ID: M6APDG00605)
Name
GM6001
Synonyms
Ilomastat; Galardin; 142880-36-2; GM 6001; Illomastat; CS 610; GM-6001; UNII-I0403ML141; CHEMBL19611; Ilomastat (GM6001, Galardin); I0403ML141; NCGC00163450-02; 3-(N-HYDROXYCARBOXAMIDO)-2-ISOBUTYLPROPANOYL-TRP-METHYLAMIDE; (R)-N4-Hydroxy-N1-[(S)-2-(1H-indol-3-yl)-1-methylcarbamoyl-ethyl]-2-isobutyl-succinamide; N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan Methylamide; (R)-N(sup 1)-Hydroxy-N-((S)-2-indol-3-yl-1-(methylcarbamoyl)ethyl)-2-isobutylsuccinamide; (S-(R*,S*))-N(sup 4)-Hydroxy-N(sup; ILOMASTAT
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Status
Discontinued in Phase 2
Structure
Formula
C20H28N4O4
InChI
1S/C20H28N4O4/c1-12(2)8-13(10-18(25)24-28)19(26)23-17(20(27)21-3)9-14-11-22-16-7-5-4-6-15(14)16/h4-7,11-13,17,22,28H,8-10H2,1-3H3,(H,21,27)(H,23,26)(H,24,25)/t13-,17+/m1/s1
InChIKey
NITYDPDXAAFEIT-DYVFJYSZSA-N
PubChem CID
132519
TTD Drug ID
D0T9HG
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 GM6001. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-1 (MMP-1). [1], [2]
Matrix metalloproteinase-12 (MMP-12)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-12 (MMP-12) is a therapeutic target for GM6001. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-12 (MMP-12). [3], [4]
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 GM6001. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [5], [6]
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 GM6001. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [6], [7]
Matrix metalloproteinase-2 (MMP-2)
E3 ubiquitin-protein ligase Hakai (CBLL1)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-2 (MMP-2) is a therapeutic target for GM6001. The E3 ubiquitin-protein ligase Hakai (CBLL1) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-2 (MMP-2). [4], [8]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-2 (MMP-2) is a therapeutic target for GM6001. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-2 (MMP-2). [4], [9]
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 GM6001. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-3 (MMP-3). [10], [11]
Matrix metalloproteinase-9 (MMP-9)
E3 ubiquitin-protein ligase Hakai (CBLL1)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-9 (MMP-9) is a therapeutic target for GM6001. The E3 ubiquitin-protein ligase Hakai (CBLL1) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-9 (MMP-9). [4], [8]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Matrix metalloproteinase-9 (MMP-9) is a therapeutic target for GM6001. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GM6001 through regulating the expression of Matrix metalloproteinase-9 (MMP-9). [3], [4]
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 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. doi: 10.1093/nar/28.1.235.
Ref 3 The aberrant cross-talk of epithelium-macrophages via METTL3-regulated extracellular vesicle miR-93 in smoking-induced emphysema. Cell Biol Toxicol. 2022 Feb;38(1):167-183. doi: 10.1007/s10565-021-09585-1. Epub 2021 Mar 4.
Ref 4 Neovastat, a naturally occurring multifunctional antiangiogenic drug, in phase III clinical trials. Semin Oncol. 2001 Dec;28(6):620-5. doi: 10.1016/s0093-7754(01)90035-1.
Ref 5 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 6 Selective matrix metalloproteinase inhibition attenuates progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Am J Physiol Heart Circ Physiol. 2006 Jun;290(6):H2522-7. doi: 10.1152/ajpheart.00932.2005. Epub 2006 Jan 20.
Ref 7 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 8 CBLL1 is highly expressed in non-small cell lung cancer and promotes cell proliferation and invasion. Thorac Cancer. 2019 Jun;10(6):1479-1488. doi: 10.1111/1759-7714.13097. Epub 2019 May 23.
Ref 9 RNA m6A methyltransferase METTL3 regulates invasiveness of melanoma cells by matrix metallopeptidase 2. Melanoma Res. 2019 Aug;29(4):382-389. doi: 10.1097/CMR.0000000000000580.
Ref 10 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 11 Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage. J Med Chem. 2015 Apr 9;58(7):2941-57. doi: 10.1021/jm501939z. Epub 2015 Feb 25.