AAN-TAT-Lipo-Dox

AAN-TAT-Lipo-Dox is an investigational, tumor-targeted, legumain protease-activated liposomal formulation of doxorubicin developed by researchers at Nankai University. It consists of liposomes loaded with the chemotherapeutic agent doxorubicin, modified on their surface with a cell-penetrating peptide (TAT) that is covalently blocked by the legumain-specific substrate Ala-Ala-Asn (AAN). In systemic circulation, the AAN moiety masks the cell-penetrating activity of TAT, reducing non-specific cellular uptake and systemic toxicity, such as cardiotoxicity. Upon reaching the tumor microenvironment, extracellular legumain—which is highly overexpressed in various solid tumors and tumor-associated macrophages—cleaves the AAN substrate. This cleavage restores the transmembrane transport function of the TAT peptide, facilitating efficient internalization of the liposomes into tumor cells and enhancing the tumoricidal efficacy of doxorubicin.

Other names

AAN-TAT-Lipo-DOXAAN-TAT-liposome-DOX