Publication in Frontiers in Pharmacology on Optimizing the Enzymatic Release of MMAE from isoDGR-based SMDC by Incorporation of a GPLG-PABC Enzymatically Cleavable Linker

As a member of Magicbullet::Reloaded Consortium, KINETO Lab took a big part in the study where the use of GPLG-PABC linker in a Small Molecule Drug Conjugates (SMDC), as an efficient lysosomal cleavable linker, is reported for the first time and, in the future, it might represent an alternative to other well-established enzymatically sensitive peptide sequences. Moreover, the antiproliferative activity of conjugate, in so called “kiss-and-run” protocol, resulted to be significantly more potent than the free MMAE, with the relative potency clearly consistent with the expression of the integrin receptor in the four cancer cell lines.

The publication can be accessed under the following link.