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

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

Arianna Amenta ¹, Susanna Comi ², Marcelo Kravicz ², Silvia Sesana ², Antonia Antoniou ³, Daniele Passarella ¹, Pierfausto Seneci ¹, Sara Pellegrino ³, Francesca Re ²

Arianna Amenta ¹, Susanna Comi ², Marcelo Kravicz ²

¹Department of Chemistry, University of Milan Milan Italy.
²School of Medicine and Surgery, University of Milano-Bicocca Monza Italy francesca.re1@unimib.it.
³Department of Pharmaceutical Sciences, University of Milan Milan Italy.

⁰Department of Chemistry, University of Milan Milan Italy.

Rsc Medicinal Chemistry +

|

October 21, 2024

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View abstract on PubMed

Summary

This summary is machine-generated.

A novel pimasertib prodrug, PROPIMA, was synthesized to enhance cancer treatment. This glutathione-responsive drug selectively inhibits melanoma cell proliferation and migration, offering improved therapeutic potential.

Area Of Science

Pharmacology
Medicinal Chemistry
Cancer Biology

Background

Pimasertib is an antiproliferative drug targeting the ERK/MAPK pathway in cancers like melanoma.
Enhancing pimasertib's tumor cell selectivity and half-life is crucial for improved therapeutic efficacy.
Prodrug design and nanodelivery systems offer potential strategies for drug improvement.

Purpose Of The Study

To synthesize and evaluate a glutathione (GSH)-responsive prodrug of pimasertib (PROPIMA).
To assess the in vitro biological activity of PROPIMA in a human melanoma cell line model.
To investigate the potential of liposomal encapsulation for PROPIMA delivery.

Main Methods

Synthesis of PROPIMA featuring a redox-sensitive disulfide linker for GSH-mediated activation.
In vitro evaluation of PROPIMA's antiproliferative and cytotoxic effects on melanoma cells.
Assessment of pERK levels and cancer cell migration inhibition by PROPIMA.

Main Results

PROPIMA demonstrated selective inhibition of melanoma cell proliferation and viability.
PROPIMA reduced pERK levels by approximately 5-fold compared to the parent drug.
Both free and liposome-encapsulated PROPIMA exhibited enhanced inhibition of cancer cell migration.

Conclusions

PROPIMA is a promising GSH-responsive prodrug of pimasertib with enhanced anti-cancer activity.
The prodrug design effectively targets cancer cells and improves drug efficacy.
Liposomal delivery of PROPIMA warrants further investigation for improved cancer therapy.

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