New research has strengthened chemotherapy drugs' ability to fight cancer cells.

Scientists from King’s College, led by Dr. Madiha Chowdhury, have successfully increased the resistance of commonly used chemotherapy drugs against proteins exploited by cancer cells called Efflux pumps. They are naturally found in the cell membrane and function as protectors of cells against harmful or unwanted substances. However, when controlled by cancer cells, they block the effects of chemotherapy drugs instead.

The study, published in the Journal of Medicinal Chemistry, shows that the proprietary technology, efflux resistance breaker (ERB), is effective at deactivating the pumps in cancer cells. This development hints at a potential solution against chemoresistance in cancer therapy.

Miraz Rahman, Professor of Medicinal Chemistry at King’s and senior author of the study, said:

“Drug resistance remains one of the greatest barriers to long-term cancer control. This study shows that by building efflux resistance directly into the drug structure, we can overcome transporter-mediated resistance without the toxicity issues that have limited previous approaches. It offers a powerful framework to redesign existing cancer drugs and make them effective again.”

For the purpose of the study, the team tested their ERB-driven design on imatinib, a tyrosine kinase inhibitor designed to treat chronic myeloid leukaemia. Despite its ability to address a rare type of cancer, imatinib is chemoresistant. It contains chemical properties that efflux pumps such as P-glycoprotein (P-gp) and the Breast Cancer Resistance Protein (BCRP) easily recognize and therefore block, minimizing the drug’s effectiveness.

Ben Forbes, Professor of Pharmaceutics at King’s and a co-author of the study, said:

“Efflux pumps such as P-gp and BCRP play a central role in limiting drug accumulation in cancer cells. This study shows that drugs can be designed to be less recognizable to efflux pumps. This allows therapeutic drug levels to build up inside the cells without having to block the pumps or interfere with other cell functions.”

By incorporating ERB chemical fragments into the drug’s core structure, the new and improved imatinib remained inside cancer cells and performed its function without being pumped out. 

This study has given the team the drive to believe that cancer treatment failure due to efflux pumps may soon be a thing of the past. The team suggests that ERB technology could be instrumental in revolutionizing the development of anticancer drugs.

Read the full article here to learn more about the ERB technology.

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