Drug Information
Drug (ID: DG01908) and It's Reported Resistant Information
Name |
DETD-35
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Synonyms |
DETD-35
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Target | . | NOUNIPROTAC | [1] |
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
Melanoma [ICD-11: 2C30]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.V600E (c.1799T>A) |
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Sensitive Disease | Melanoma [ICD-11: 2C30.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | MEK/ERK signaling pathway | Inhibition | hsa04011 | |
AKT signaling pathway | Inhibition | hsa04151 | ||
STAT3 signaling pathway | Inhibition | hsa04550 | ||
In Vitro Model | A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 |
MeWo cells | Skin | Homo sapiens (Human) | CVCL_0445 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
B16-F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
SkMEL2 cells | Skin | Homo sapiens (Human) | CVCL_0069 | |
BRAF cells | N.A. | Homo sapiens (Human) | N.A. | |
In Vivo Model | NSG mouse PDX model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis; Immunohistochemistry analysis | |||
Experiment for Drug Resistance |
MTT assay; Crystal violet staining assay; FACS assay | |||
Mechanism Description | DETD-35 overcame acquired vemurafenib resistance at least in part through deregulating MEK-ERK, Akt, and STAT3 signaling pathways and promoting apoptosis of cancer cells. |
References
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