Drug Information

Drug (ID: DG01714) and It's Reported Resistant Information

• Name: ACY-957/GSK126
• Synonyms: ACY-957/GSK126
• Target: .; NOUNIPROTAC; [1]

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Diffuse large B-cell lymphoma [ICD-11: 2A81]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: Histone-lysine N-methyltransferase EZH2 (EZH2) [1]

• Molecule Alteration: Missense mutation; p.Y641N (c.1921T>A)
• Sensitive Disease: Diffuse large B-cell lymphoma [ICD-11: 2A81.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Hela cells; Cervix uteri; Homo sapiens (Human); CVCL_0030
• Experiment for Molecule Alteration: Chromatin Immunoprecipitation assay; Western blotting analysis
• Experiment for Drug Resistance: Propidium-iodide cell cycle analysis; BrdU-PI cell cycle analysis

Key Molecule: Histone-lysine N-methyltransferase EZH2 (EZH2) [1]

• Molecule Alteration: Missense mutation; p.Y641N (c.1921T>A)
• Sensitive Disease: Diffuse large B-cell lymphoma [ICD-11: 2A81.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: Hela cells; Cervix uteri; Homo sapiens (Human); CVCL_0030
• Experiment for Molecule Alteration: Chromatin Immunoprecipitation assay; Western blotting analysis
• Experiment for Drug Resistance: Propidium-iodide cell cycle analysis; BrdU-PI cell cycle analysis

References

• Ref 1: HDAC1,2 inhibition impairs EZH2- and BBAP-mediated DNA repair to overcome chemoresistance in EZH2 gain-of-function mutant diffuse large B-cell lymphomaOncotarget. 2015 Mar 10;6(7):4863-87. doi: 10.18632/oncotarget.3120.