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Association details:
| Biomarker: | GNA11 mutation |
|---|---|
| Cancer: | Uveal Melanoma |
| Drug: | elesclomol (STA-4783) (Apoptosis stimulant, Reactive oxygen species stimulant, HSP70 stimulant) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Copper ionophore elesclomol selectively targets GNAQ/11-mutant uveal melanoma
Published date:
06/13/2022
Excerpt:
Elesclomol was identified in a differential cytotoxicity screen of an in-house tool compound library, and its in vivo pharmacological efficacy was further confirmed in zebrafish and mouse UM models. Mechanistically, elesclomol transports copper to mitochondria and produces a large amount of reactive oxygen species (ROS) as Cu(II) is reduced to Cu(I) in GNAQ/11-mutant UM cells...Elesclomol may provide a new therapeutic path for selectively targeting malignant GNAQ/11-mutant UM.
DOI:
10.1038/s41388-022-02364-0
