Lysine-based cell-penetrating peptides for intracellular delivery

Applications: Pharmaceuticals, biopharmaceuticals, drug delivery, RNA therapeutics, bioimaging, diagnostics, gene therapy

Using lysine instead of arginine in cell-penetrating peptides (CPP’s) creates a delivery vehicle with different properties to the CPP – ASO conjugates in clinical trials. High levels of correction can be achieved with improved delivery and reduced toxicity.

Features	Benefits
Synthetic CPP suitable for delivery of a range of small and large molecules.	Can deliver nucleotides, peptides, small molecules, or antibodies intracellularly.
Exon-skipping correction leads to wild-type levels of expression in disease models.	Effective disease modification in vivo.
The efficacy of this class of peptides is driven purely by lysine, with no arginine in the peptide.	This results in different characteristics compared to CPP’s in the clinic, and can therefore provide an alternative efficacy and toxicity profile.
Effective biodistribution.	High levels of delivery to tissues throughout the body, including improved muscle, heart and brain delivery.
Different toxicity profile to peptides in the clinic.	Overcomes issues seen with other CPP’s. The data shows that the nephrotoxicity associated with arginine-based CPP’s is unlikely.
Wider therapeutic window compared to arginine-CPP’s.	Reduced dosage required and therefore costs.

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Lysine-based cell-penetrating peptides for intracellular delivery

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