Targeting the creatine transporter SLC6A8: Mechanisms and emerging therapeutic strategies for multiple diseases - PubMed
3 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.