System X_c^- Antiporter Inhibitors: Azo-Linked Amino-Naphthyl-Sulfonate Analogues of Sulfasalazine.

ABSTRACT: The cystine/glutamate antiporter system X_c^- (SX_c^-) mediates the exchange of intracellular L-glutamate (L-Glu) with extracellular L-cystine (L-Cys₂). Both the import of L-Cys₂ and the export of L-Glu take on added significance in CNS cells, especially astrocytes. When the relative activity of SX_c^- overwhelms the regulatory capacity of the EAATs, the efflux of L-Glu through the antiporter can be significant enough to trigger excitotoxic pathology, as is thought to occur in glioblastoma. This has prompted considerable interest in the pharmacological specificity of SX_c^- and the development of inhibitors. The present study explores a series of analogues that are structurally related to

SUBMITTER: Nehser M 

PROVIDER: S-EPMC10688270 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature