{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Cirillo D"],"funding":["Department of Biomedicine at the University of Bergen","European Commission"],"pagination":["2650-2668"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8518981"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["16(17)"],"pubmed_abstract":["The xCT antiporter is a cell membrane protein involved in active counter-transportation of glutamate (outflux) with cystine (influx) over the human cell membrane. This feature makes the xCT antiporter a crucial element of the biosynthesis of the vital free radical scavenger glutathione. The prodrug sulfasalazine, a medication for the treatment of ulcerative colitis, was previously proven to inhibit the xCT antiporter. Starting from sulfasalazine, a molecular scaffold jumping followed by SAR-assisted design and synthesis provided a series of styryl hydroxy-benzoic acid analogues that were biologically tested in vitro for their ability to decrease intracellular glutathione levels using four different cancer cell lines: A172 (glioma), A375 (melanoma), U87 (glioma) and MCF7 (breast carcinoma)."],"journal":["ChemMedChem"],"pubmed_title":["Structure-Activity-Relationship-Aided Design and Synthesis of xCT Antiporter Inhibitors."],"pmcid":["PMC8518981"],"funding_grant_id":["675417"],"pubmed_authors":["Oyvind Enger P","Bjorsvik HR","Cirillo D","Sarowar S"],"additional_accession":[]},"is_claimable":false,"name":"Structure-Activity-Relationship-Aided Design and Synthesis of xCT Antiporter Inhibitors.","description":"The xCT antiporter is a cell membrane protein involved in active counter-transportation of glutamate (outflux) with cystine (influx) over the human cell membrane. This feature makes the xCT antiporter a crucial element of the biosynthesis of the vital free radical scavenger glutathione. The prodrug sulfasalazine, a medication for the treatment of ulcerative colitis, was previously proven to inhibit the xCT antiporter. Starting from sulfasalazine, a molecular scaffold jumping followed by SAR-assisted design and synthesis provided a series of styryl hydroxy-benzoic acid analogues that were biologically tested in vitro for their ability to decrease intracellular glutathione levels using four different cancer cell lines: A172 (glioma), A375 (melanoma), U87 (glioma) and MCF7 (breast carcinoma).","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Sep","modification":"2025-04-04T09:18:39.242Z","creation":"2025-04-04T09:18:39.242Z"},"accession":"S-EPMC8518981","cross_references":{"pubmed":["33847044"],"doi":["10.1002/cmdc.202100204"]}}