A novel, glutathione-activated prodrug of pimasertib loaded in liposomes for targeted cancer therapy.

ABSTRACT: Pimasertib, a potent antiproliferative drug, has been extensively studied for treating cancers characterized by dysregulation in the ERK/MAPK signaling pathway, such as melanoma. However, its therapeutic efficacy would greatly benefit from an increased selectivity for tumour cells and a longer half-life. Such improvements may be achieved by combining the rational design of a prodrug with its encapsulation in a potential nanodelivery system. For this reason, we synthesized a glutathione (GSH)-responsive putative prodrug of pimasertib (PROPIMA), which contains a redox-sensitive disulphide linker that can be processed by GSH to activate pimasertib. The synthesis of PROPIMA and its in vitro biological activity on a human melanoma cell line as a model are described. The results showed th

SUBMITTER: Amenta A 

PROVIDER: S-EPMC11485093 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature