Enhancer ID: | E_01_0127 |
Species: | human |
Position : | chr7:148804439-148806439 |
Biosample name: | |
Experiment class : | High+Lowthroughput |
Enhancer type: | Enhancer |
Disease: | Cancer |
Pubmed ID: | 31819273 |
Enhancer experiment: | Western blot, cell viability assay, crystal violet staining, QRT PCR |
Enhancer experiment description: | Using a hydrophobic tagging approach, we generated MS1943, a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. Importantly, MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells, and is efficacious in vivo, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2. |
Target gene : | -- |
Strong evidence: | qRT-PCR,qPCR,ChIP,3C |
Less strong evidence: | RNA-Seq |
Target gene experiment description: | Using a hydrophobic tagging approach, we generated MS1943, a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. Importantly, MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells, and is efficacious in vivo, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2. |
TF name : | EZH2(ENX-1,ENX1b,KMT6,KMT6A,WVS,WVS2,EZH2) |
TF experiment: | western blot??????????????qRT-PCR |
TF experiment description: | Using a hydrophobic tagging approach, we generated MS1943, a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. Importantly, MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells, and is efficacious in vivo, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2. |
Enhancer function : | Using a hydrophobic tagging approach, we generated MS1943, a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. Importantly, MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells, and is efficacious in vivo, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2. |
Enhancer function experiment: | Immunohistochemical staining |
Enhancer function experiment description: |
Using a hydrophobic tagging approach, we generated MS1943, a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. Importantly, MS1943 has a profound cytotoxic effect in multiple TNBC cells, while sparing normal cells, and is efficacious in vivo, suggesting that pharmacologic degradation of EZH2 can be advantageous for treating the cancers that are dependent on EZH2. |
SNP ID: | -- |
GeneName | Pathway Name | Source | Gene Number |
---|---|---|---|
EZH2 | Activation of anterior HOX genes in hindbrain development during early embryogenesis | reactome | 120 |
EZH2 | Oxidative Stress Induced Senescence | reactome | 120 |
EZH2 | PKMTs methylate histone lysines | reactome | 64 |
EZH2 | PRC2 methylates histones and DNA | reactome | 71 |
EZH2 | Hs_Endoderm_Differentiation_WP2853_88152 | wikipathways | 62 |
EZH2 | Hs_Interactome_of_polycomb_repressive_complex_2_(PRC2)_WP2916_88672 | wikipathways | 15 |