m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG01403)
Name
RS-130830
Synonyms
CTS-1027; 193022-04-7; RS-130830; UNII-2QD3F58224; CHEMBL440498; 2QD3F58224; 4-[4-(4-CHLORO-PHENOXY)-BENZENESULFONYLMETHYL]-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HYDROXYAMIDE; 4-[[[4-(4-Chlorophenoxy)phenyl]sulfonyl]methyl]tetrahydro-N-hydroxy-2H-pyran-4-carboxamide; 4-(4-(4-Chloro-phenoxy)-benzenesulfonylmethyl)-tetrahydro-pyran-4-carboxylic acid hydroxyamide; Ro-1130830; AC1MOE9A; SCHEMBL2381112; BDBM11863; DTXSID90172907; 830c; CTS 1027; ZINC1488366; BCP13018; 3563AH; alpha-tetrahydropyran beta-sulfone 1B; AKOS030526690
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Status
Discontinued in Phase 2
Structure
Formula
C19H20ClNO6S
InChI
1S/C19H20ClNO6S/c20-14-1-3-15(4-2-14)27-16-5-7-17(8-6-16)28(24,25)13-19(18(22)21-23)9-11-26-12-10-19/h1-8,23H,9-13H2,(H,21,22)
InChIKey
ROSNVSQTEGHUKU-UHFFFAOYSA-N
PubChem CID
3342298
TTD Drug ID
D03BOZ
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
 Regulator Info 
Response Summary Matrix metalloproteinase-1 (MMP-1) is a therapeutic target for RS-130830. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RS-130830 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
 Regulator Info 
Response Summary Matrix metalloproteinase-13 (MMP-13) is a therapeutic target for RS-130830. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of RS-130830 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
 Regulator Info 
Response Summary Matrix metalloproteinase-13 (MMP-13) is a therapeutic target for RS-130830. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RS-130830 through regulating the expression of Matrix metalloproteinase-13 (MMP-13). [4], [5]
Matrix metalloproteinase-2 (MMP-2)
E3 ubiquitin-protein ligase Hakai (CBLL1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Matrix metalloproteinase-2 (MMP-2) is a therapeutic target for RS-130830. The E3 ubiquitin-protein ligase Hakai (CBLL1) has potential in affecting the response of RS-130830 through regulating the expression of Matrix metalloproteinase-2 (MMP-2). [6], [7]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Matrix metalloproteinase-2 (MMP-2) is a therapeutic target for RS-130830. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RS-130830 through regulating the expression of Matrix metalloproteinase-2 (MMP-2). [7], [8]
Matrix metalloproteinase-3 (MMP-3)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Matrix metalloproteinase-3 (MMP-3) is a therapeutic target for RS-130830. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RS-130830 through regulating the expression of Matrix metalloproteinase-3 (MMP-3). [9], [10]
Matrix metalloproteinase-9 (MMP-9)
E3 ubiquitin-protein ligase Hakai (CBLL1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Matrix metalloproteinase-9 (MMP-9) is a therapeutic target for RS-130830. The E3 ubiquitin-protein ligase Hakai (CBLL1) has potential in affecting the response of RS-130830 through regulating the expression of Matrix metalloproteinase-9 (MMP-9). [6], [7]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Matrix metalloproteinase-9 (MMP-9) is a therapeutic target for RS-130830. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RS-130830 through regulating the expression of Matrix metalloproteinase-9 (MMP-9). [7], [11]
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 Phase 1/2 trial of BMS-275291 in patients with human immunodeficiency virus-related Kaposi sarcoma: a multicenter trial of the AIDS Malignancy Consortium. Cancer. 2008 Mar 1;112(5):1083-8. doi: 10.1002/cncr.23108.
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 Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6529-34. doi: 10.1016/j.bmcl.2007.09.085. Epub 2007 Sep 29.
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.
Ref 6 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 7 Inhibitory effect of DA-125, a new anthracyclin analog antitumor agent, on the invasion of human fibrosarcoma cells by down-regulating the matrix metalloproteinases. Biochem Pharmacol. 2005 Dec 19;71(1-2):21-31. doi: 10.1016/j.bcp.2005.10.007. Epub 2005 Nov 2.
Ref 8 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 9 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 10 Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1', Bioorg. Med. Chem. Lett. 5(6):539-542 (1995).
Ref 11 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.