m6A-centered Drug Response Information
General Information of the Drug (ID: M6ADRUG0107)
| Name |
Imatinib
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| Synonyms |
Cgp 57148; Glamox; Glamox (TN); Gleevec (TN); Glivec (TN); Imatinib (INN); Imatinib (STI571); Imatinib Methansulfonate; Imatinib [INN:BAN]; 112GI019; 152459-95-5; BKJ8M8G5HI; CCRIS 9076; CGP-57148; CHEMBL941; Imatinib free base; STI; UNII-BKJ8M8G5HI
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| Status | Approved | [1] | |||
| Structure |
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| Formula |
C29H31N7O
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| InChI |
InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
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| InChIKey |
KTUFNOKKBVMGRW-UHFFFAOYSA-N
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Full List of m6A Targets Related to This Drug
Multidrug resistance-associated protein 1 (MRP1/ABCC1)
| In total 1 item(s) under this target gene | ||||
| Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [2] | |||
| Response Summary | METTL3, and the YTHDF1/eEF-1 complex mediate the translation of Multidrug resistance-associated protein 1 (MRP1/ABCC1) mRNA in an m6A-dependent manner to regulate the intracellular concentration of imatinib and drug resistance of gastrointestinal stromal tumor (GIST). | |||
| Responsed Disease | Gastrointestinal stromal tumour | ICD-11: 2B5B | ||
| Target Regulator | Methyltransferase-like 3 (METTL3) | WRITER | ||
| Target Regulation | Up regulation | |||
| In-vitro Model | GIST-T1 | Gastrointestinal stromal tumor | Homo sapiens | CVCL_4976 |
| GIST882 | Gastrointestinal stromal tumor | Homo sapiens | CVCL_7044 | |
| In-vivo Model | For tumor growth assay, 4 × 106 logarithmically growing GIST cells were transfected with T1S-vector, T1S-METTL3, 882S-vector, or 882S-METTL3 constructs, and subcutaneously injected in 100 ul of PBS into the flank of female nude mice(4-week-old). Mice were then randomly divided into 8 groups (n = 5 in each group): (1) injected with T1S-vector-harboring cells, and treated with imatinib (600 mg/l in drinking water); (2) injected with T1S-vector-harboring cells, and treated with imatinib (600 mg/l in drinking water) and MRP1 inhibitor (100 mg/l in drinking water); (3) injected with T1S-METTL3-harboring cells, and treated with imatinib (600 mg/l in drinking water); (4) injected with T1S-METTL3-harboring cells, and treated with imatinib (600 mg/l in drinking water) and MRP1 inhibitor (100 mg/l in drinking water); (5) injected with 882S-vector-harboring cells and treated with imatinib (600 mg/l in drinking water); (6) injected with 882S-vector-harboring cells, and treated with imatinib (600 mg/l in drinking water) and MRP1 inhibitor (100 mg/l in drinking water); (7) injected with 882S-METTL3-harboring cells, and treated with imatinib (600 mg/l in drinking water); and (8) injected with 882S-METTL3-harboring cells, and treated with imatinib (600 mg/l in drinking water) and MRP1 inhibitor (100 mg/l in drinking water). | |||
References