Drug Information
Drug (ID: DG00017) and It's Reported Resistant Information
Name |
Vinorelbine
|
||||
---|---|---|---|---|---|
Synonyms |
Eunades; Exelbine; NVB; Navelbine; Vinorelbin; Vinorelbina; Vinorelbinum; Navelbine base; Vinorelbina [Spanish]; Vinorelbine Ditartarate; Vinorelbine ditartrate; Vinorelbine tartrate; Vinorelbinum [Latin]; KW 2307; KW 2307 base; ANX-530; KW-2307; Navelbine (TN); SDP-012; Vinorelbine (INN); Vinorelbine [INN:BAN]; Aspidospermidine-3-carboxylic acid; Nor-5'-anhydrovinblastine; Methyl (2beta,3beta,4beta,5alpha,12beta,19alpha)-4-acetoxy-15-[(6R,8S)-4-ethyl-8-(methoxycarbonyl)-1,3,6,7,8,9-hexahydro-2,6-methanoazecino[4,3-b]indol-8-yl]-3-hydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidine-3-carboxylate; Methyl (2b,3b,4b,5a,12b,19a)-4-(acetyloxy)-15-[(6R,8S)-4-ethyl-8-(methoxycarbonyl)-1,3,6,7,8,9-hexahydro-2,6-methanoazecino[4,3-b]indol-8-yl]-3-hydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidine-3-carboxylate
Click to Show/Hide
|
||||
Indication |
In total 1 Indication(s)
|
||||
Structure | |||||
Drug Resistance Disease(s) |
Disease(s) with Clinically Reported Resistance for This Drug
(1 diseases)
Pleural mesothelioma [ICD-11: 2C26]
[2]
Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug
(1 diseases)
Esophageal cancer [ICD-11: 2B70]
[1]
|
||||
Target | Tubulin (TUB) | NOUNIPROTAC | [1] | ||
Click to Show/Hide the Molecular Information and External Link(s) of This Drug | |||||
Formula |
C45H54N4O8
|
||||
IsoSMILES |
CCC1=C[C@H]2C[C@@](C3=C(CN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)[C@]78CCN9[C@H]7[C@@](C=CC9)([C@H]([C@@]([C@@H]8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC
|
||||
InChI |
1S/C45H54N4O8/c1-8-27-19-28-22-44(40(51)55-6,36-30(25-48(23-27)24-28)29-13-10-11-14-33(29)46-36)32-20-31-34(21-35(32)54-5)47(4)38-43(31)16-18-49-17-12-15-42(9-2,37(43)49)39(57-26(3)50)45(38,53)41(52)56-7/h10-15,19-21,28,37-39,46,53H,8-9,16-18,22-25H2,1-7H3/t28-,37-,38+,39+,42+,43+,44-,45-/m0/s1
|
||||
InChIKey |
GBABOYUKABKIAF-IELIFDKJSA-N
|
||||
PubChem CID | |||||
ChEBI ID | |||||
TTD Drug ID | |||||
VARIDT ID | |||||
DrugBank ID |
Type(s) of Resistant Mechanism of This Drug
EADR: Epigenetic Alteration of DNA, RNA or Protein
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Esophageal cancer [ICD-11: 2B70]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Epigenetic Alteration of DNA, RNA or Protein (EADR) | ||||
Key Molecule: hsa-miR-193a-3p | [1] | |||
Molecule Alteration | Expression | Up-regulation |
||
Resistant Disease | Esophageal cancer [ICD-11: 2B70.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | Cell apoptosis | Inhibition | hsa04210 | |
Cell proliferation | Activation | hsa05200 | ||
In Vitro Model | KYSE150 cells | Esophagus | Homo sapiens (Human) | CVCL_1348 |
KYSE510 cells | Esophagus | Homo sapiens (Human) | CVCL_1354 | |
kYSE410 cells | Esophagus | Homo sapiens (Human) | CVCL_1352 | |
kYSE450 cells | Esophagus | Homo sapiens (Human) | CVCL_1353 | |
In Vivo Model | Nude mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | Over-expression of miR-193a-3p increased the radioresistance and chemoresistance of oesophageal squamous cell carcinoma (ESCC) cells. In contrast, the down-regulation of miR-193a-3p decreased the radioresistance and chemoresistance of ESCC cells. In addition, miR-193a-3p inducing DNA damage has also been demonstrated through measuring the level of gamma-H2AX associated with miR-193a-3p. Moreover, a small interfering RNA(siRNA)-induced repression of the PSEN1 gene had an effect similar to that of miR-193a-3p up-regulation. The above processes also inhibited oesophageal cancer cells apoptosis. These findings suggest that miR-193a-3p contributes to the radiation and chemotherapy resistance of oesophageal carcinoma by down-regulating PSEN1. | |||
Key Molecule: hsa-miR-193a-3p | [1] | |||
Molecule Alteration | Expression | Up-regulation |
||
Resistant Disease | Esophageal cancer [ICD-11: 2B70.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | KYSE150 cells | Esophagus | Homo sapiens (Human) | CVCL_1348 |
KYSE510 cells | Esophagus | Homo sapiens (Human) | CVCL_1354 | |
kYSE410 cells | Esophagus | Homo sapiens (Human) | CVCL_1352 | |
kYSE450 cells | Esophagus | Homo sapiens (Human) | CVCL_1353 | |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | Over-expression of miR-193a-3p increased the radioresistance and chemoresistance of oesophageal squamous cell carcinoma (ESCC) cells. The regulation role of miR-193a-3p on multi-chemoresistance and radioresistance were mediated by PSEN1. | |||
Key Molecule: hsa-miR-193a-3p | [1] | |||
Molecule Alteration | Expression | Up-regulation |
||
Resistant Disease | Esophageal cancer [ICD-11: 2B70.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | KYSE150 cells | Esophagus | Homo sapiens (Human) | CVCL_1348 |
KYSE510 cells | Esophagus | Homo sapiens (Human) | CVCL_1354 | |
kYSE410 cells | Esophagus | Homo sapiens (Human) | CVCL_1352 | |
kYSE450 cells | Esophagus | Homo sapiens (Human) | CVCL_1353 | |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | Over-expression of miR-193a-3p increased the radioresistance and chemoresistance of oesophageal squamous cell carcinoma (ESCC) cells. The regulation role of miR-193a-3p on multi-chemoresistance and radioresistance were mediated by PSEN1. | |||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Presenilin-1 (PSEN1) | [1] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Esophageal cancer [ICD-11: 2B70.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | Cell apoptosis | Inhibition | hsa04210 | |
Cell proliferation | Activation | hsa05200 | ||
In Vitro Model | KYSE150 cells | Esophagus | Homo sapiens (Human) | CVCL_1348 |
KYSE510 cells | Esophagus | Homo sapiens (Human) | CVCL_1354 | |
kYSE410 cells | Esophagus | Homo sapiens (Human) | CVCL_1352 | |
kYSE450 cells | Esophagus | Homo sapiens (Human) | CVCL_1353 | |
Experiment for Molecule Alteration |
Western blot analysis | |||
Experiment for Drug Resistance |
MTT assay | |||
Mechanism Description | Over-expression of miR-193a-3p increased the radioresistance and chemoresistance of oesophageal squamous cell carcinoma (ESCC) cells. In contrast, the down-regulation of miR-193a-3p decreased the radioresistance and chemoresistance of ESCC cells. In addition, miR-193a-3p inducing DNA damage has also been demonstrated through measuring the level of gamma-H2AX associated with miR-193a-3p. Moreover, a small interfering RNA(siRNA)-induced repression of the PSEN1 gene had an effect similar to that of miR-193a-3p up-regulation. The above processes also inhibited oesophageal cancer cells apoptosis. These findings suggest that miR-193a-3p contributes to the radiation and chemotherapy resistance of oesophageal carcinoma by down-regulating PSEN1. |
Pleural mesothelioma [ICD-11: 2C26]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Epigenetic Alteration of DNA, RNA or Protein (EADR) | ||||
Key Molecule: hsa-mir-15a | [2] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Malignant pleural mesothelioma [ICD-11: 2C26.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | MSTO-211H cells | Lung | Homo sapiens (Human) | CVCL_1430 |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
SYBR Green-based assay | |||
Mechanism Description | Expression of miR-15a, miR-16 and miR-34a was downregulated in MPM cells with acquired drug resistance. Transfection with miR-15a or miR-16 mimics reversed the resistance to cisplatin, gemcitabine or vinorelbine, whereas miR-34a reversed cisplatin and vinorelbine resistance only. | |||
Key Molecule: hsa-mir-15a | [2] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Malignant pleural mesothelioma [ICD-11: 2C26.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | MSTO-211H cells | Lung | Homo sapiens (Human) | CVCL_1430 |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
SYBR Green-based assay | |||
Mechanism Description | Expression of miR-15a, miR-16 and miR-34a was downregulated in MPM cells with acquired drug resistance. Transfection with miR-15a or miR-16 mimics reversed the resistance to cisplatin, gemcitabine or vinorelbine, whereas miR-34a reversed cisplatin and vinorelbine resistance only. | |||
Key Molecule: hsa-mir-16 | [2] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Malignant pleural mesothelioma [ICD-11: 2C26.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | MSTO-211H cells | Lung | Homo sapiens (Human) | CVCL_1430 |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
SYBR Green-based assay | |||
Mechanism Description | Expression of miR-15a, miR-16 and miR-34a was downregulated in MPM cells with acquired drug resistance. Transfection with miR-15a or miR-16 mimics reversed the resistance to cisplatin, gemcitabine or vinorelbine, whereas miR-34a reversed cisplatin and vinorelbine resistance only. | |||
Key Molecule: hsa-mir-16 | [2] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Malignant pleural mesothelioma [ICD-11: 2C26.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | MSTO-211H cells | Lung | Homo sapiens (Human) | CVCL_1430 |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
SYBR Green-based assay | |||
Mechanism Description | Expression of miR-15a, miR-16 and miR-34a was downregulated in MPM cells with acquired drug resistance. Transfection with miR-15a or miR-16 mimics reversed the resistance to cisplatin, gemcitabine or vinorelbine, whereas miR-34a reversed cisplatin and vinorelbine resistance only. | |||
Key Molecule: Forkhead box protein O3 (FOXO3) | [2] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Malignant pleural mesothelioma [ICD-11: 2C26.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | MSTO-211H cells | Lung | Homo sapiens (Human) | CVCL_1430 |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
SYBR Green-based assay | |||
Mechanism Description | Expression of miR-15a, miR-16 and miR-34a was downregulated in MPM cells with acquired drug resistance. Transfection with miR-15a or miR-16 mimics reversed the resistance to cisplatin, gemcitabine or vinorelbine, whereas miR-34a reversed cisplatin and vinorelbine resistance only. | |||
Key Molecule: Forkhead box protein O3 (FOXO3) | [2] | |||
Molecule Alteration | Expression | Down-regulation |
||
Resistant Disease | Malignant pleural mesothelioma [ICD-11: 2C26.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | MSTO-211H cells | Lung | Homo sapiens (Human) | CVCL_1430 |
Experiment for Molecule Alteration |
qRT-PCR | |||
Experiment for Drug Resistance |
SYBR Green-based assay | |||
Mechanism Description | Expression of miR-15a, miR-16 and miR-34a was downregulated in MPM cells with acquired drug resistance. Transfection with miR-15a or miR-16 mimics reversed the resistance to cisplatin, gemcitabine or vinorelbine, whereas miR-34a reversed cisplatin and vinorelbine resistance only. |
References
If you find any error in data or bug in web service, please kindly report it to Dr. Sun and Dr. Zhang.