Pub. Date : 2021
PMID : 33995089
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Case Report: 7-Ethyl-10-Hydroxycamptothecin, a DNA Topoisomerase I Inhibitor, Performs BRD4 Inhibitory Activity and Inhibits Human Leukemic Cell Growth. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 2 | In our study, SN-38 was characterized as a potent and reversible BRD4 inhibitor [IC50 = 660.2 nM against BRD4 (BD1) and IC50 = 547.7 nM against BRD4 (BD2)] in biochemical assay using drug repurposing strategy. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 3 | In our study, SN-38 was characterized as a potent and reversible BRD4 inhibitor [IC50 = 660.2 nM against BRD4 (BD1) and IC50 = 547.7 nM against BRD4 (BD2)] in biochemical assay using drug repurposing strategy. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 4 | In our study, SN-38 was characterized as a potent and reversible BRD4 inhibitor [IC50 = 660.2 nM against BRD4 (BD1) and IC50 = 547.7 nM against BRD4 (BD2)] in biochemical assay using drug repurposing strategy. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 5 | Additional cellular assay suggested that SN-38 can bind BRD4 in human leukemic cell K562 and inhibit cell growth with IC50 = 0.2798 muM in a BRD4 dependent manner partially. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 6 | Additional cellular assay suggested that SN-38 can bind BRD4 in human leukemic cell K562 and inhibit cell growth with IC50 = 0.2798 muM in a BRD4 dependent manner partially. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 7 | Additionally, mechanism study indicated that SN-38 can induce the accumulation of BRD4 substrate c-Myc and cleavage of caspase 3. | Irinotecan | bromodomain containing 4 | Homo sapiens |
| 8 | In sum, our findings identified BRD4 as a new target of SN-38 and reveals SN-38 as a modifier of histone acetylation reader for the first time, which may provide a new insight for further optimization of dual target inhibitor. | Irinotecan | bromodomain containing 4 | Homo sapiens |