Invited
Blood-brain barrier bhuttle peptides, from discovery to applications

Gate2Brain shuttle peptides represent salvage for new or previously rejected CNS drug candidates by providing a way to cross the blood-brain barrier (BBB).

Gate2Brain technology consist on a toolbox of peptides able to cross the BBB and carry compounds covalently attached (including small molecules, peptides, proteins, antibodies, plasmids, siRNA or mRNA loaded nanoparticles, etc…) that cannot cross this barrier unaided. They have proofed to carry these cargoes in vitro and in vivo. These peptide shuttles use the existing transport mechanisms at the BBB without affecting the normal functioning of these mechanisms and preserving brain homeostasis.

By improving the delivery of therapeutic candidate to the CNS, we will ensure immediate impact in many CNS diseases patients. In addition, in a broader perspective, Gate2Brain technology may help to repurpose existing therapies previously rejected because of difficulty to reach the brain, accelerating the translation towards clinical development. Gate2Brain will also result in the application of lower concentrations of therapeutic agent, thereby significantly lowering systemic side effects and reducing the cost of the treatment.

Gate2Brain peptides combine protease resistance, capacity to carry a wide range of cargoes thanks to their versatility, low production costs, and low immunogenic risk. They provide a non-invasive, non-antigenic, permeable, stable, soluble and receptor-specific way to transport drugs across the BBB and into the CNS.

References:

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2. M. Sánchez-Navarro et al. Curr. Opin. Chem. Biol. (2017), 38, 134-140.
3. M. Sánchez-Navarro et al. Acc. Chem. Res. (2017), 50, 1847-1854.
4. R. Prades et al. Angew. Chem. Int. Ed. (2015), 54, 3967-3972.
5. B. Oller-Salvia et al. Angew. Chem. Int. Ed. (2016), 55, 572-575.