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Targeting the creatine transporter SLC6A8: Mechanisms and emerging therapeutic strategies for multiple diseases - PubMed

5 hours ago
  • #Therapeutic target
  • #Disease mechanism
  • #Creatine metabolism
  • SLC6A8 is a sodium- and chloride-dependent creatine transporter essential for maintaining intracellular creatine levels and cellular energy balance.
  • Dysregulation of SLC6A8 is associated with creatine transporter deficiency (CTD), various cancers, diabetes, obesity, and heart failure.
  • Conventional creatine supplementation is ineffective for most CTD patients, but emerging strategies like gene therapy, small-molecule correctors, and lipophilic prodrugs show promise in preclinical models.
  • SLC6A8 is overexpressed in multiple cancers, and its inhibitor RGX-202 (β-GPA) exhibits antitumor effects in preclinical colorectal and hepatocellular carcinoma models.
  • The review highlights SLC6A8's role in neurological disorders, cancer, and other diseases, emphasizing its potential as a therapeutic target.