2022
DOI: 10.1016/j.bioorg.2022.105829
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Development of novel androgen receptor antagonists based on the structure of darolutamide

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Cited by 2 publications
(3 citation statements)
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“…To investigate the binding mode of GA32 with AR or GR, the molecular docking was performed using the DOCK module in the molecular modeling package molecular operating environment (MOE). To date, the crystal structure of AR-LBD in the antagonistic form has not been resolved, and the antagonistic model of AR-LBD (PDB-ID: 1Z95) was constructed as previously described through molecular modeling 4MDD).…”
Section: Resultsmentioning
confidence: 99%
See 1 more Smart Citation
“…To investigate the binding mode of GA32 with AR or GR, the molecular docking was performed using the DOCK module in the molecular modeling package molecular operating environment (MOE). To date, the crystal structure of AR-LBD in the antagonistic form has not been resolved, and the antagonistic model of AR-LBD (PDB-ID: 1Z95) was constructed as previously described through molecular modeling 4MDD).…”
Section: Resultsmentioning
confidence: 99%
“…To date, the crystal structure of AR-LBD in the antagonistic form has not been resolved, and the antagonistic model of AR-LBD (PDB-ID: 1Z95) was constructed as previously described through molecular modeling. 25 GA32 was docked into the HBP site of the AR-LBD model as well as that of the GR-LBD structure (PDB-ID: 4MDD). Molecular dynamics simulations were further performed to explore the more accurate interaction model between GA32 and AR or GR (Figure S3).…”
Section: ■ Introductionmentioning
confidence: 99%
“…It is not yet clear whether combination therapy of low dose of TRC-253 with other androgen inhibitors such as abiraterone can lower its toxicity and improve the anti-tumor effect. A more recent study has developed several AR antagonists based on the structure of darolutamide, from which "compound 28t" has been found to show superior efficacy against two resistant mutants (AR-F876L and AR-T877A) relative to darolutamide [53]. Further clinical trials are needed to assess its safety, pharmacokinetics, and efficiency.…”
Section: Emerging Ar Antagonists In Clinical Trialsmentioning
confidence: 99%