m6A-centered Drug Response Information
General Information of the Drug (ID: M6ADRUG0003)
| Name |
Chloroquine
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| Synonyms |
Amokin; Aralen; Aralen HCl; Arechin; Arechine; Arequin; Arolen; Arthrochin; Artrichin; Avlochlor; Avloclor; Bemaco; Bemaphate; Bemasulph; Benaquin; Bipiquin; CU-01000012392-2; Capquin; Chemochin; Chingamin; Chloraquine; Chlorochin; Chlorochine; Chlorochinum; Chloroin; Chloroquin; Chloroquina; Chloroquine (USP/INN); Chloroquine (VAN); Chloroquine Bis-Phosphoric Acid; Chloroquine FNA (TN); Chloroquine [USAN:INN:BAN]; Chloroquine phosphate; Chloroquinium; Chloroquinum; Chloroquinum [INN-Latin]; Chlorquin; Cidanchin; Clorochina; Clorochina [DCIT]; Cloroquina; Cloroquina [INN-Spanish]; Cocartrit; Dawaquin (TN); Delagil; Dichinalex; Elestol; Gontochin; Gontochin phosphate; Heliopar; Imagon; Ipsen 225; Iroquine; Khingamin; Klorokin; Lapaquin; Malaquin; Malaquin (*Diphosphate*); Malaren; Malarex; Mesylith; Miniquine; Neochin; Nivachine; Nivaquine B; Pfizerquine; Quinachlor; Quinagamin; Quinagamine; Quinercyl; Quingamine; Quinilon; Quinoscan; RP 3377; RP-3377; Resochen; Resochin; Resochin (TN); Resoquina; Resoquine; Reumachlor; Reumaquin; Rivoquine; Ro 01-6014/N2; Ronaquine; Roquine; SN 6718; SN-7618; ST 21; ST 21 (pharmaceutical); Sanoquin; Silbesan;Siragan; Solprina; Sopaquin; Tanakan; Tanakene; Tresochin; Trochin; W 7618;WIN 244
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| Status | Approved | [1] | |||
| Structure |
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| Formula |
C18H26ClN3
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| InChI |
InChI=1S/C18H26ClN3/c1-4-22(5-2)12-6-7-14(3)21-17-10-11-20-18-13-15(19)8-9-16(17)18/h8-11,13-14H,4-7,12H2,1-3H3,(H,20,21)
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| InChIKey |
WHTVZRBIWZFKQO-UHFFFAOYSA-N
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Full List of m6A Targets Related to This Drug
Autophagy protein 5 (ATG5)
| 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 could positively regulate the autophagy by targeting the autophagy-related genes such as Autophagy protein 5 (ATG5), ATG7, LC3B, and SQSTM1. beta-elemene inhibited the autophagy flux by preventing autophagic lysosome acidification, resulting in increasing expression of SQSTM1 and LC3B-II. beta-elemene could reverse gefitinib resistance in non-small cell lung cancer cells by inhibiting cell autophagy process in a manner of chloroquine. METTL3-mediated autophagy in reversing gefitinib resistance of NSCLC cells by beta-elemene, which shed light on providing potential molecular-therapy target and clinical-treatment method in NSCLC patients with gefitinib resistance. | |||
| Responsed Disease | Non-small-cell lung carcinoma | ICD-11: 2C25.Y | ||
| Target Regulator | Methyltransferase-like 3 (METTL3) | WRITER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | Autophagy | hsa04140 | ||
| Cell Process | Autophagic lysosome acidification | |||
| In-vitro Model | Gefitinib-resistant cell line HCC827GR (Gefitinib-resistant HCC827 cell line) | |||
| Gefitinib-resistant cell line PC9GR (Gefitinib-resistant PC9 cell line) | ||||
| HCC827 | Lung adenocarcinoma | Homo sapiens | CVCL_2063 | |
| PC-9 | Lung adenocarcinoma | Homo sapiens | CVCL_B260 | |
| In-vivo Model | NSCLC gefitinib-resistant cells (5 × 106 cells in 100 uL PBS) were injected subcutaneously into the lateral surface of the left abdomen of 6-week-old female BALB/c nude mice (at least five mice per group to ensure accuracy). | |||
Cyclic AMP-dependent transcription factor ATF-4 (ATF4)
| In total 2 item(s) under this target gene | ||||
| Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [3] | |||
| Response Summary | In colorectal cancer, Glutaminolysis inhibition upregulated ATF4 expression in an m6A-dependent manner to activate pro-survival autophagy through transcriptional activation of the mTOR inhibitor DDIT4. Determined the relationship between FTO alpha-ketoglutarate dependent dioxygenase (FTO), YTH N6-methyladenosine RNA binding protein 2 (YTHDF2), and ATF4. Cyclic AMP-dependent transcription factor ATF-4 (ATF4) transcriptionally upregulated DDIT4 to suppress mTOR, which induced pro-survival autophagy during glutaminolysis inhibition. | |||
| Responsed Disease | Colorectal cancer | ICD-11: 2B91 | ||
| Target Regulator | YTH domain-containing family protein 2 (YTHDF2) | READER | ||
| Target Regulation | Down regulation | |||
| Pathway Response | mTOR signaling pathway | hsa04150 | ||
| Cell Process | RNA decay | |||
| Cell growth and death | ||||
| Cell autophagy | ||||
| In-vitro Model | HCT 116 | Colon carcinoma | Homo sapiens | CVCL_0291 |
| SW480 | Colon adenocarcinoma | Homo sapiens | CVCL_0546 | |
| Experiment 2 Reporting the m6A-centered Drug Response by This Target Gene | [3] | |||
| Response Summary | In colorectal cancer, Glutaminolysis inhibition upregulated ATF4 expression in an m6A-dependent manner to activate pro-survival autophagy through transcriptional activation of the mTOR inhibitor DDIT4. Determined the relationship between FTO alpha-ketoglutarate dependent dioxygenase (FTO), YTH N6-methyladenosine RNA binding protein 2 (YTHDF2), and ATF4. ATF4 transcriptionally upregulated DDIT4 to suppress Cyclic AMP-dependent transcription factor ATF-4 (ATF4), which induced pro-survival autophagy during glutaminolysis inhibition. | |||
| Responsed Disease | Colorectal cancer | ICD-11: 2B91 | ||
| Target Regulator | Fat mass and obesity-associated protein (FTO) | ERASER | ||
| Pathway Response | mTOR signaling pathway | hsa04150 | ||
| Cell Process | RNA decay | |||
| Cell growth and death | ||||
| Cell autophagy | ||||
| In-vitro Model | HCT 116 | Colon carcinoma | Homo sapiens | CVCL_0291 |
| SW480 | Colon adenocarcinoma | Homo sapiens | CVCL_0546 | |
Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B/LC3B-II)
| 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 could positively regulate the autophagy by targeting the autophagy-related genes such as ATG5, ATG7, LC3B, and SQSTM1. beta-elemene inhibited the autophagy flux by preventing autophagic lysosome acidification, resulting in increasing expression of SQSTM1 and Microtubule-associated proteins 1A/1B light chain 3B (MAP1LC3B/LC3B-II). beta-elemene could reverse gefitinib resistance in non-small cell lung cancer cells by inhibiting cell autophagy process in a manner of chloroquine. METTL3-mediated autophagy in reversing gefitinib resistance of NSCLC cells by beta-elemene, which shed light on providing potential molecular-therapy target and clinical-treatment method in NSCLC patients with gefitinib resistance. | |||
| Responsed Disease | Non-small-cell lung carcinoma | ICD-11: 2C25.Y | ||
| Target Regulator | Methyltransferase-like 3 (METTL3) | WRITER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | Autophagy | hsa04140 | ||
| Cell Process | Autophagic lysosome acidification | |||
| In-vitro Model | Gefitinib-resistant cell line HCC827GR (Gefitinib-resistant HCC827 cell line) | |||
| Gefitinib-resistant cell line PC9GR (Gefitinib-resistant PC9 cell line) | ||||
| HCC827 | Lung adenocarcinoma | Homo sapiens | CVCL_2063 | |
| PC-9 | Lung adenocarcinoma | Homo sapiens | CVCL_B260 | |
| In-vivo Model | NSCLC gefitinib-resistant cells (5 × 106 cells in 100 uL PBS) were injected subcutaneously into the lateral surface of the left abdomen of 6-week-old female BALB/c nude mice (at least five mice per group to ensure accuracy). | |||
Sequestosome-1 (SQSTM1)
| 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 could positively regulate the autophagy by targeting the autophagy-related genes such as ATG5, ATG7, LC3B, and Sequestosome-1 (SQSTM1). beta-elemene inhibited the autophagy flux by preventing autophagic lysosome acidification, resulting in increasing expression of SQSTM1 and LC3B-II. beta-elemene could reverse gefitinib resistance in non-small cell lung cancer cells by inhibiting cell autophagy process in a manner of chloroquine. METTL3-mediated autophagy in reversing gefitinib resistance of NSCLC cells by beta-elemene, which shed light on providing potential molecular-therapy target and clinical-treatment method in NSCLC patients with gefitinib resistance. | |||
| Responsed Disease | Non-small-cell lung carcinoma | ICD-11: 2C25.Y | ||
| Target Regulator | Methyltransferase-like 3 (METTL3) | WRITER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | Autophagy | hsa04140 | ||
| Cell Process | Autophagic lysosome acidification | |||
| In-vitro Model | Gefitinib-resistant cell line HCC827GR (Gefitinib-resistant HCC827 cell line) | |||
| Gefitinib-resistant cell line PC9GR (Gefitinib-resistant PC9 cell line) | ||||
| HCC827 | Lung adenocarcinoma | Homo sapiens | CVCL_2063 | |
| PC-9 | Lung adenocarcinoma | Homo sapiens | CVCL_B260 | |
| In-vivo Model | NSCLC gefitinib-resistant cells (5 × 106 cells in 100 uL PBS) were injected subcutaneously into the lateral surface of the left abdomen of 6-week-old female BALB/c nude mice (at least five mice per group to ensure accuracy). | |||
Serine/threonine-protein kinase mTOR (MTOR)
| In total 2 item(s) under this target gene | ||||
| Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [3] | |||
| Response Summary | In colorectal cancer, Glutaminolysis inhibition upregulated ATF4 expression in an m6A-dependent manner to activate pro-survival autophagy through transcriptional activation of the mTOR inhibitor DDIT4. Determined the relationship between FTO alpha-ketoglutarate dependent dioxygenase (FTO), YTH N6-methyladenosine RNA binding protein 2 (YTHDF2), and ATF4. Serine/threonine-protein kinase mTOR (MTOR) transcriptionally upregulated DDIT4 to suppress mTOR, which induced pro-survival autophagy during glutaminolysis inhibition. | |||
| Responsed Disease | Colorectal cancer | ICD-11: 2B91 | ||
| Target Regulator | YTH domain-containing family protein 2 (YTHDF2) | READER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | mTOR signaling pathway | hsa04150 | ||
| Autophagy | hsa04140 | |||
| Cell Process | RNA decay | |||
| Cell growth and death | ||||
| Cell autophagy | ||||
| In-vitro Model | HCT 116 | Colon carcinoma | Homo sapiens | CVCL_0291 |
| SW480 | Colon adenocarcinoma | Homo sapiens | CVCL_0546 | |
| Experiment 2 Reporting the m6A-centered Drug Response by This Target Gene | [3] | |||
| Response Summary | In colorectal cancer, Glutaminolysis inhibition upregulated ATF4 expression in an m6A-dependent manner to activate pro-survival autophagy through transcriptional activation of the mTOR inhibitor DDIT4. Determined the relationship between FTO alpha-ketoglutarate dependent dioxygenase (FTO), YTH N6-methyladenosine RNA binding protein 2 (YTHDF2), and ATF4. ATF4 transcriptionally upregulated DDIT4 to suppress Serine/threonine-protein kinase mTOR (MTOR), which induced pro-survival autophagy during glutaminolysis inhibition. | |||
| Responsed Disease | Colorectal cancer | ICD-11: 2B91 | ||
| Target Regulator | Fat mass and obesity-associated protein (FTO) | ERASER | ||
| Pathway Response | mTOR signaling pathway | hsa04150 | ||
| Autophagy | hsa04140 | |||
| Cell Process | RNA decay | |||
| Cell growth and death | ||||
| Cell autophagy | ||||
| In-vitro Model | HCT 116 | Colon carcinoma | Homo sapiens | CVCL_0291 |
| SW480 | Colon adenocarcinoma | Homo sapiens | CVCL_0546 | |
Ubiquitin-like modifier-activating enzyme ATG7 (ATG7)
| 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 could positively regulate the autophagy by targeting the autophagy-related genes such as ATG5, Ubiquitin-like modifier-activating enzyme ATG7 (ATG7), LC3B, and SQSTM1. beta-elemene inhibited the autophagy flux by preventing autophagic lysosome acidification, resulting in increasing expression of SQSTM1 and LC3B-II. beta-elemene could reverse gefitinib resistance in non-small cell lung cancer cells by inhibiting cell autophagy process in a manner of chloroquine. METTL3-mediated autophagy in reversing gefitinib resistance of NSCLC cells by beta-elemene, which shed light on providing potential molecular-therapy target and clinical-treatment method in NSCLC patients with gefitinib resistance. | |||
| Responsed Disease | Non-small-cell lung carcinoma | ICD-11: 2C25.Y | ||
| Target Regulator | Methyltransferase-like 3 (METTL3) | WRITER | ||
| Target Regulation | Up regulation | |||
| Pathway Response | Autophagy | hsa04140 | ||
| Cell Process | Autophagic lysosome acidification | |||
| In-vitro Model | Gefitinib-resistant cell line HCC827GR (Gefitinib-resistant HCC827 cell line) | |||
| Gefitinib-resistant cell line PC9GR (Gefitinib-resistant PC9 cell line) | ||||
| HCC827 | Lung adenocarcinoma | Homo sapiens | CVCL_2063 | |
| PC-9 | Lung adenocarcinoma | Homo sapiens | CVCL_B260 | |
| In-vivo Model | NSCLC gefitinib-resistant cells (5 × 106 cells in 100 uL PBS) were injected subcutaneously into the lateral surface of the left abdomen of 6-week-old female BALB/c nude mice (at least five mice per group to ensure accuracy). | |||
References