Drug Information
Drug (ID: DG01226) and It's Reported Resistant Information
| Name |
Verteporfin
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| Synonyms |
Visudyne (TN); SCHEMBL6218; Verteporfin (JAN/USP/INN); SCHEMBL1230373; Verteporfin, >=94% (HPLC); HY-B0146; AKOS015896072; AKOS037515819; CS-1950; D01162; Verteporfin, United States Pharmacopeia (USP) Reference Standard
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| Indication |
In total 1 Indication(s)
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| Structure |
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| Target | . | NOUNIPROTAC | [1] | ||
| Click to Show/Hide the Molecular Information and External Link(s) of This Drug | |||||
| Formula |
C82H84N8O16
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| IsoSMILES |
CC1=C(C2=CC3=NC(=CC4=C(C(=C(N4)C=C5[C@@]6([C@@H](C(=CC=C6C(=N5)C=C1N2)C(=O)OC)C(=O)OC)C)C)CCC(=O)OC)C(=C3C)CCC(=O)O)C=C.CC1=C(C2=CC3=NC(=CC4=C(C(=C(N4)C=C5[C@@]6([C@@H](C(=CC=C6C(=N5)C=C1N2)C(=O)OC)C(=O)OC)C)C)CCC(=O)O)C(=C3C)CCC(=O)OC)C=C
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| InChI |
1S/2C41H42N4O8/c1-9-23-20(2)29-17-34-27-13-10-26(39(49)52-7)38(40(50)53-8)41(27,5)35(45-34)19-30-22(4)24(11-14-36(46)47)32(44-30)18-33-25(12-15-37(48)51-6)21(3)28(43-33)16-31(23)42-29;1-9-23-20(2)29-17-34-27-13-10-26(39(49)52-7)38(40(50)53-8)41(27,5)35(45-34)19-30-22(4)25(12-15-37(48)51-6)33(44-30)18-32-24(11-14-36(46)47)21(3)28(43-32)16-31(23)42-29/h2*9-10,13,16-19,38,42,44H,1,11-12,14-15H2,2-8H3,(H,46,47)/t2*38-,41+/m00/s1
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| InChIKey |
NJLRKAMQPVVOIU-IDLGWYNRSA-N
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Type(s) of Resistant Mechanism of This Drug
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Prostate cancer [ICD-11: 2C82]
| Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
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Unusual Activation of Pro-survival Pathway (UAPP)
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| Key Molecule: Myb-related protein B (MYBL2) | [1] | |||
| Molecule Alteration | Expression | Down-regulation |
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| Sensitive Disease | Prostate cancer [ICD-11: 2C82.0] | |||
| Experimental Note | Revealed Based on the Cell Line Data | |||
| In Vitro Model | HEp-2 cells | Skin | Homo sapiens (Human) | CVCL_1906 |
| U251 cells | Brain | Homo sapiens (Human) | CVCL_0021 | |
| BT474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
| A172 cells | Brain | Homo sapiens (Human) | CVCL_0131 | |
| U87 cells | Brain | Homo sapiens (Human) | CVCL_0022 | |
| H1299 cells | Lung | Homo sapiens (Human) | CVCL_0060 | |
| Calu-3 cells | Lung | Homo sapiens (Human) | CVCL_0609 | |
| HuTu80 cells | Small intestine | Homo sapiens (Human) | CVCL_1301 | |
| In Vivo Model | Male BALB/c nude mouse model | Mus musculus | ||
| Experiment for Molecule Alteration |
Western blotting analysis; qRT-PCR | |||
| Experiment for Drug Resistance |
WST-1 assay; Colony formation assay; Annexin V-FITC/PI Apoptosis assay | |||
| Mechanism Description | MYBL2 expression was significantly upregulated in CRPC tissues and cell lines. Overexpression of MYBL2 could facilitate castration-resistant growth and metastatic capacity in androgen-dependent PCa cells by promoting YAP1 transcriptional activity via modulating the activity of the Rho GTPases RhoA and LATS1 kinase. Importantly, targeting MYBL2, or treatment with either the YAP/TAZ inhibitor Verteporfin or the RhoA inhibitor Simvastatin, reversed the resistance to ADT and blocked bone metastasis in CRPC cells. | |||
| Key Molecule: Transcriptional coactivator YAP1 (YAP1) | [1] | |||
| Molecule Alteration | Expression | Down-regulation |
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| Sensitive Disease | Prostate cancer [ICD-11: 2C82.0] | |||
| Experimental Note | Revealed Based on the Cell Line Data | |||
| In Vitro Model | HEp-2 cells | Skin | Homo sapiens (Human) | CVCL_1906 |
| U251 cells | Brain | Homo sapiens (Human) | CVCL_0021 | |
| BT474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
| A172 cells | Brain | Homo sapiens (Human) | CVCL_0131 | |
| U87 cells | Brain | Homo sapiens (Human) | CVCL_0022 | |
| H1299 cells | Lung | Homo sapiens (Human) | CVCL_0060 | |
| Calu-3 cells | Lung | Homo sapiens (Human) | CVCL_0609 | |
| HuTu80 cells | Small intestine | Homo sapiens (Human) | CVCL_1301 | |
| In Vivo Model | Male BALB/c nude mouse model | Mus musculus | ||
| Experiment for Molecule Alteration |
Western blotting analysis; qRT-PCR | |||
| Experiment for Drug Resistance |
WST-1 assay; Colony formation assay; Annexin V-FITC/PI Apoptosis assay | |||
| Mechanism Description | MYBL2 expression was significantly upregulated in CRPC tissues and cell lines. Overexpression of MYBL2 could facilitate castration-resistant growth and metastatic capacity in androgen-dependent PCa cells by promoting YAP1 transcriptional activity via modulating the activity of the Rho GTPases RhoA and LATS1 kinase. Importantly, targeting MYBL2, or treatment with either the YAP/TAZ inhibitor Verteporfin or the RhoA inhibitor Simvastatin, reversed the resistance to ADT and blocked bone metastasis in CRPC cells. | |||
Uveal melanoma [ICD-11: 2D0Y]
| Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
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Unusual Activation of Pro-survival Pathway (UAPP)
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| Key Molecule: Guanine nucleotide-binding protein alpha-q (GNAQ) | [2] | |||
| Molecule Alteration | Missense mutation | p.Q209L (c.626A>T) |
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| Sensitive Disease | Uveal melanoma [ICD-11: 2D0Y.0] | |||
| Experimental Note | Revealed Based on the Cell Line Data | |||
| Cell Pathway Regulation | Hippo signaling pathway | Inhibition | hsa04390 | |
| In Vivo Model | Nude mouse PDX model | Mus musculus | ||
References
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