Drug Information

Drug (ID: DG01737) and It's Reported Resistant Information

• Name: APR-246/Cisplatin
• Synonyms: APR-246/Cisplatin
• Target: .; NOUNIPROTAC; [1]

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

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Cellular tumor antigen p53 (TP53) [1]

• Molecule Alteration: Missense mutation; p.R248W (c.742C>T)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A2780-CP20 cells; Ovary; Homo sapiens (Human); CVCL_A5PS
• In Vivo Model: Female CD-1 Nu/Nu mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay; WST-1 assay; Cell Titer-Glo assay; MTS assay

Key Molecule: Cellular tumor antigen p53 (TP53) [1]

• Molecule Alteration: Missense mutation; p.R273H (c.818G>A)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A2780-CP20 cells; Ovary; Homo sapiens (Human); CVCL_A5PS
• In Vivo Model: Female CD-1 Nu/Nu mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay; WST-1 assay; Cell Titer-Glo assay; MTS assay

Key Molecule: Cellular tumor antigen p53 (TP53) [1]

• Molecule Alteration: Missense mutation; p.Y163C (c.488A>G)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A2780-CP20 cells; Ovary; Homo sapiens (Human); CVCL_A5PS
• In Vivo Model: Female CD-1 Nu/Nu mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay; WST-1 assay; Cell Titer-Glo assay; MTS assay

Peritoneal cancer [ICD-11: 2C51]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.C135Y (c.404G>A)
• Sensitive Disease: Peritoneal cancer [ICD-11: 2C51.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

Ovarian cancer [ICD-11: 2C73]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.L111Q (c.332T>A)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.P151H (c.452C>A)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.Y163H (c.487T>C)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.P278R (c.833C>G)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.R280K (c.839G>A)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Cellular tumor antigen p53 (TP53) [1]

• Molecule Alteration: Missense mutation; p.R248Q (c.743G>A)
• Sensitive Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: A2780-CP20 cells; Ovary; Homo sapiens (Human); CVCL_A5PS
• In Vivo Model: Female CD-1 Nu/Nu mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay; WST-1 assay; Cell Titer-Glo assay; MTS assay

Fallopian tube cancer [ICD-11: 2C74]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Cellular tumor antigen p53 (TP53) [2]

• Molecule Alteration: Missense mutation; p.C238F (c.713G>T)
• Sensitive Disease: Fallopian tube cancer [ICD-11: 2C74.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ascitic fluid; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: FMCA assay

References

• Ref 1: APR-246 overcomes resistance to cisplatin and doxorubicin in ovarian cancer cellsCell Death Dis. 2015 Jun 18;6(6):e1794. doi: 10.1038/cddis.2015.143.
• Ref 2: Strong synergy with APR-246 and DNA-damaging drugs in primary cancer cells from patients with TP53 mutant High-Grade Serous ovarian cancerJ Ovarian Res. 2016 May 14;9(1):27. doi: 10.1186/s13048-016-0239-6.