Drug Information

Drug (ID: DG01886) and It's Reported Resistant Information

• Name: Anti-estrogens
• Synonyms: Anti-estrogens
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Breast cancer [ICD-11: 2C60]; [1]
• Target: .; NOUNIPROTAC; [2]

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

Breast cancer [ICD-11: 2C60]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Estrogen receptor alpha (ESR1) [2]

• Molecule Alteration: Missense mutation; p.P535H (c.1604C>A)
• Resistant Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: MDA-MB-231cells; Breast; Homo sapiens (Human); CVCL_0062
• In Vitro Model: ZR75-1 cells; Breast; Homo sapiens (Human); CVCL_0588
• In Vitro Model: MDA-MB-361 cells; Breast; Homo sapiens (Human); CVCL_0620
• In Vitro Model: MDA-MB-231cells; Breast; Homo sapiens (Human); CVCL_0062
• In Vitro Model: SkBR3 MCF7 cells; Breast; Homo sapiens (Human); N.A.
• In Vitro Model: MCF Tet-On cells; Pleural effusion; Homo sapiens (Human); CVCL_V332
• In Vitro Model: Ishikawa cells; Endometrium; Homo sapiens (Human); CVCL_2529
• In Vitro Model: MCF Tet-On cells; Pleural effusion; Homo sapiens (Human); CVCL_V332
• In Vivo Model: Nu/Nu athymic BALB/c female mouse model; Mus musculus
• Experiment for Molecule Alteration: IMPACT assay; Western blotting analysis; Luciferase assays; Microarrays assay
• Experiment for Drug Resistance: MSKCC assay

Key Molecule: Estrogen receptor alpha (ESR1) [1]

• Molecule Alteration: Missense mutation; p.E380Q (c.1138G>C)
• Resistant Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Identified from the Human Clinical Data

Key Molecule: Estrogen receptor alpha (ESR1) [1]

• Molecule Alteration: Missense mutation; p.L536X (c.1606_1608)
• Resistant Disease: Breast adenocarcinoma [ICD-11: 2C60.1]
• Experimental Note: Identified from the Human Clinical Data

References

• Ref 1: Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nat Genet. 2013 Dec;45(12):1446-51. doi: 10.1038/ng.2823. Epub 2013 Nov 3.
• Ref 2: ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nat Genet. 2013 Dec;45(12):1439-45. doi: 10.1038/ng.2822. Epub 2013 Nov 3.