Drug Information

Drug (ID: DG01895) and It's Reported Resistant Information
Name
ERBB2 TKIs
Synonyms
ERBB2 TKIs
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Target . NOUNIPROTAC [1]
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
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Solid tumour/cancer [ICD-11: 2A00-2F9Z]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.G309E (c.926G>A)
 Molecule Info 
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.G309E (c.926G>A) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.S310Y (c.929C>A)
 Molecule Info 
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.S310Y (c.929C>A) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.S310F (c.929C>T)
 Molecule Info 
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.S310F (c.929C>T) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.C311R (c.931T>C)
 Molecule Info 
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.C311R (c.931T>C) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]
Molecule Alteration Missense mutation
p.E321G (c.962A>G)
 Molecule Info 
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model NIH 3T3 cells Colon Homo sapiens (Human) CVCL_0594
Experiment for
Drug Resistance		 WST-1 assay
Mechanism Description The missense mutation p.E321G (c.962A>G) in gene ERBB2 cause the sensitivity of ERBB2 TKIs by aberration of the drug's therapeutic target
References
Ref 1 Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14476-81. doi: 10.1073/pnas.1203201109. Epub 2012 Aug 20.

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