General Information of the Drug (ID: M6APDG01985)
Name
KT-5720
Synonyms
KT 5720; KT5720; 108068-98-0; GTPL337; ZINC3873013; KT 5720, > hexyl (15R,16R,18S)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8,10,12,20,22,24-nonaene-16-carboxylate; (9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3 inverted exclamation marka,2 inverted exclamation marka,1 inverted exclamation marka-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-c
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Status
Investigative
Structure
Formula
C32H31N3O5
InChI
1S/C32H31N3O5/c1-3-4-5-10-15-39-30(37)32(38)16-23-34-21-13-8-6-11-18(21)25-26-20(17-33-29(26)36)24-19-12-7-9-14-22(19)35(28(24)27(25)34)31(32,2)40-23/h6-9,11-14,23,38H,3-5,10,15-17H2,1-2H3,(H,33,36)/t23-,31+,32+/m0/s1
InChIKey
ZHEHVZXPFVXKEY-RUAOOFDTSA-N
PubChem CID
454202
TTD Drug ID
D0G2VC
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.
Extracellular signal-regulated kinase 2 (ERK2)
Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
In total 1 mechanisms lead to this potential drug response
Response Summary Extracellular signal-regulated kinase 2 (ERK2) is a therapeutic target for KT-5720. The Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) has potential in affecting the response of KT-5720 through regulating the expression of Extracellular signal-regulated kinase 2 (ERK2). [1], [2]
Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)
In total 1 mechanisms lead to this potential drug response
Response Summary Extracellular signal-regulated kinase 2 (ERK2) is a therapeutic target for KT-5720. The Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) has potential in affecting the response of KT-5720 through regulating the expression of Extracellular signal-regulated kinase 2 (ERK2). [2], [3]
YTH domain-containing family protein 3 (YTHDF3)
In total 1 mechanisms lead to this potential drug response
Response Summary Extracellular signal-regulated kinase 2 (ERK2) is a therapeutic target for KT-5720. The YTH domain-containing family protein 3 (YTHDF3) has potential in affecting the response of KT-5720 through regulating the expression of Extracellular signal-regulated kinase 2 (ERK2). [2], [3]
Ribosomal protein S6 kinase beta-1 (S6K1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Ribosomal protein S6 kinase beta-1 (S6K1) is a therapeutic target for KT-5720. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of KT-5720 through regulating the expression of Ribosomal protein S6 kinase beta-1 (S6K1). [4], [5]
Stress-activated protein kinase 2a (p38 alpha)
Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase 2a (p38 alpha) is a therapeutic target for KT-5720. The Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) has potential in affecting the response of KT-5720 through regulating the expression of Stress-activated protein kinase 2a (p38 alpha). [3], [6]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase 2a (p38 alpha) is a therapeutic target for KT-5720. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of KT-5720 through regulating the expression of Stress-activated protein kinase 2a (p38 alpha). [6], [7]
YTH domain-containing family protein 3 (YTHDF3)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase 2a (p38 alpha) is a therapeutic target for KT-5720. The YTH domain-containing family protein 3 (YTHDF3) has potential in affecting the response of KT-5720 through regulating the expression of Stress-activated protein kinase 2a (p38 alpha). [3], [6]
Stress-activated protein kinase JNK1 (JNK1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase JNK1 (JNK1) is a therapeutic target for KT-5720. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of KT-5720 through regulating the expression of Stress-activated protein kinase JNK1 (JNK1). [8], [9]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Stress-activated protein kinase JNK1 (JNK1) is a therapeutic target for KT-5720. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of KT-5720 through regulating the expression of Stress-activated protein kinase JNK1 (JNK1). [9], [10]
References
Ref 1 hnRNPA2B1 Promotes Colon Cancer Progression via the MAPK Pathway. Front Genet. 2021 Sep 22;12:666451. doi: 10.3389/fgene.2021.666451. eCollection 2021.
Ref 2 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 3 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 4 m(6)A methyltransferase METTL3 promotes retinoblastoma progression via PI3K/AKT/mTOR pathway. J Cell Mol Med. 2020 Oct 8;24(21):12368-78. doi: 10.1111/jcmm.15736. Online ahead of print.
Ref 5 Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55. doi: 10.1042/BJ20101024.
Ref 6 Mitogen-activated protein kinases in innate immunity. Nat Rev Immunol. 2013 Sep;13(9):679-92. doi: 10.1038/nri3495. Epub 2013 Aug 19.
Ref 7 m(6)A methyltransferase METTL3 suppresses colorectal cancer proliferation and migration through p38/ERK pathways. Onco Targets Ther. 2019 Jun 4;12:4391-4402. doi: 10.2147/OTT.S201052. eCollection 2019.
Ref 8 METTL3 regulates alternative splicing of MyD88 upon the lipopolysaccharide-induced inflammatory response in human dental pulp cells. J Cell Mol Med. 2018 May;22(5):2558-2568. doi: 10.1111/jcmm.13491. Epub 2018 Mar 4.
Ref 9 Corchorusin-D directed apoptosis of K562 cells occurs through activation of mitochondrial and death receptor pathways and suppression of AKT/PKB pathway. Cell Physiol Biochem. 2012;30(4):915-26. doi: 10.1159/000341469. Epub 2012 Sep 12.
Ref 10 Post-translational modification of RNA m6A demethylase ALKBH5 regulates ROS-induced DNA damage response. Nucleic Acids Res. 2021 Jun 4;49(10):5779-5797. doi: 10.1093/nar/gkab415.