Pt(IV)-M13

Pt(IV)-M13 is a blood-brain barrier (BBB)-penetrant peptide-drug conjugate (PDC) designed for the treatment of glioblastoma (GBM). It consists of M13, a perfluoroaryl-stapled (macrocyclic) variant of the cell-penetrating peptide TP10, covalently linked to a platinum(IV) prodrug of cisplatin via an amide bond. The conjugate is designed to bypass the BBB and blood-tumor barrier (BTB) to deliver platinum specifically to brain tumor tissues. Once inside the cell, the Pt(IV) prodrug undergoes intracellular reduction to release active cisplatin, which induces DNA damage (quantified by γH2AX foci) and subsequent apoptosis. Research indicates that Pt(IV)-M13 significantly increases platinum accumulation in brain tumors compared to cisplatin alone and shows synergistic effects when combined with kinase inhibitors like 6-bromo-indirubin-3’-acetoxime (BIA).

Other names

platinum (IV)-conjugated fluorinated macrocyclic cell-penetrating peptidemacrocyclic peptide-platinum(IV) conjugate