How a brain medicine gets inside cells
Cyclocreatine Transport by SLC6A8, the Creatine Transporter, in HEK293 Cells, a Human Blood-Brain Barrier Model Cell, and CCDSs Patient-Derived Fibroblasts
Not medical advice. For informational purposes only. Always consult a healthcare professional. Terms
Surprising Findings
Cyclocreatine uses the same transporter as creatine despite being a synthetic analog.
Many drug analogs are designed to bypass defective transporters, so finding that cyclocreatine still depends on SLC6A8 is unexpected—especially since the goal was to treat SLC6A8 deficiency.
Practical Takeaways
Cyclocreatine may be a candidate for treating cerebral creatine deficiency syndromes—if the patient has some remaining creatine transporter function.
Not medical advice. For informational purposes only. Always consult a healthcare professional. Terms
Surprising Findings
Cyclocreatine uses the same transporter as creatine despite being a synthetic analog.
Many drug analogs are designed to bypass defective transporters, so finding that cyclocreatine still depends on SLC6A8 is unexpected—especially since the goal was to treat SLC6A8 deficiency.
Practical Takeaways
Cyclocreatine may be a candidate for treating cerebral creatine deficiency syndromes—if the patient has some remaining creatine transporter function.
Publication
Journal
Pharmaceutical Research
Year
2020
Authors
Tatsuki Uemura, S. Ito, Takeshi Masuda, Hiroko Shimbo, T. Goto, H. Osaka, T. Wada, P. Couraud, S. Ohtsuki
Related Content
Claims (4)
Cells use a special pump to create a sodium imbalance outside and inside the cell, and that imbalance acts like a battery to help pull creatine into the cell through a specific door called SLC6A8.
Cyclocreatine gets into brain-like cells in a lab mainly using a special doorway called the creatine transporter — when scientists block or remove this doorway, less cyclocreatine gets in, suggesting it relies on that path.
In people with a rare brain disorder caused by a broken creatine transporter, their cells don't take in creatine or a similar molecule called cyclocreatine as well — showing the broken transporter affects both in the same way.
Cyclocreatine gets into kidney cells in a way that looks like it's being actively carried in, not just drifting in on its own—kind of like being carried through a door instead of seeping through a wall.