Pub. Date : 2019 Sep 1
PMID : 30828788
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models. | darolutamide | androgen receptor | Homo sapiens |
| 2 | Darolutamide is a novel androgen receptor (AR) antagonist with a distinct chemical structure compared to other AR antagonists and currently in clinical Phase 3 trials for prostate cancer. | darolutamide | androgen receptor | Homo sapiens |
| 3 | Darolutamide is a novel androgen receptor (AR) antagonist with a distinct chemical structure compared to other AR antagonists and currently in clinical Phase 3 trials for prostate cancer. | darolutamide | androgen receptor | Homo sapiens |
| 4 | Darolutamide is a novel androgen receptor (AR) antagonist with a distinct chemical structure compared to other AR antagonists and currently in clinical Phase 3 trials for prostate cancer. | darolutamide | androgen receptor | Homo sapiens |
| 5 | Using cell-based transactivation assays, we demonstrate that darolutamide, its diastereomers and its main metabolite keto-darolutamide are strong, competitive antagonists for AR wild type, and also for several mutants identified in prostate cancer patients for which other AR antagonists show reduced antagonism or even agonism. | darolutamide | androgen receptor | Homo sapiens |
| 6 | Using cell-based transactivation assays, we demonstrate that darolutamide, its diastereomers and its main metabolite keto-darolutamide are strong, competitive antagonists for AR wild type, and also for several mutants identified in prostate cancer patients for which other AR antagonists show reduced antagonism or even agonism. | darolutamide | androgen receptor | Homo sapiens |
| 7 | Molecular modeling suggests that the flexibility of darolutamide allows accommodation in the W742C/L mutated AR ligand-binding pocket while for enzalutamide the loss of the important hydrophobic interaction with W742 leads to reduced AR interaction. | darolutamide | androgen receptor | Homo sapiens |
| 8 | Molecular modeling suggests that the flexibility of darolutamide allows accommodation in the W742C/L mutated AR ligand-binding pocket while for enzalutamide the loss of the important hydrophobic interaction with W742 leads to reduced AR interaction. | darolutamide | androgen receptor | Homo sapiens |