Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin α_vβ₆ Binding Peptide-Drug Conjugate for Tumor Targeted Drug Delivery.

ABSTRACT: Many anticancer drugs exhibit high systemic off-target toxicities causing severe side effects. Peptide-drug conjugates (PDCs) that target tumor-specific receptors such as integrin α_vβ₆ are emerging as powerful tools to overcome these challenges. The development of an integrin α_vβ₆-selective PDC was achieved by combining the therapeutic efficacy of the cytotoxic drug monomethyl auristatin E with the selectivity of the α_vβ₆-binding peptide (α_vβ₆-BP) and with the ability of positron emission tomography (PET) imaging by copper-64. The [⁶⁴Cu]PDC-1 was produced efficiently and in high purity. The PDC exhibited high human serum stability, integrin α_vβ₆-selective internal

SUBMITTER: Davis RA 

PROVIDER: S-EPMC10388305 | biostudies-literature | 2023 Jul

REPOSITORIES: biostudies-literature