Schulze FJ, Asadian-Birjand M, Pradela M, Niesler N, Nagal G, Fuchs H, (2024) A cleavable peptide adapter augments the activity of targeted toxins in combination with the glycosidic endosomal escape enhancer SO1861. BMC Biotechnol 24 doi: 10.1186/s12896-024-00854-5 PMID: 38685061
Objective: To examine whether the addition of the molecular adapter, that consists of a cell penetrating peptide and two cleavable peptides, further augments the endosomal escape enhancement of the glycosylated triterpenoid SO1861, which has shown up to more than 1000‑fold enhancement in the past.
Summary: Introducing the peptide adapter into the targeted toxin led to an about 12‑fold enhancement in the cytotoxicity on target cells while SO1861 caused a 430‑fold increase. However, the combination of adapter and glycosylated triterpenoid resulted in a more than 4300‑fold enhancement and in addition to a 51‑fold gain in specificity.
Usage: When inserting the adapter A2 between the ribosome-inactivating protein, saporin (PR-01) and the targeting moiety EGF (Saporin-A2-EGF), an improved anti-cancer effect in mice with EGFR-positive tumors and simultaneously lesser side effects were observed in comparison to Saporin-EGF.
Related Products: Saporin (Cat. #PR-01)