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Method to Screen Multidrug Transport Inhibitors Using Yeast Overexpressing a Human MDR Transporter
Laura Fiorini1, Isabelle Mus-Veteau2
1Institut de Pharmacologie Moléculaire et Cellulaire, UMR 7275 CNRS, Université de Nice-Sophia Antipolis, 660 route des Lucioles, 06560, Sophia Antipolis, Valbonne, France.
Abstract:
Multidrug resistance has appeared to mitigate the efficiency of anticancer drugs and the possibility of successful cancer chemotherapy. The Hedgehog receptor Patched is a multidrug transporter expressed in several cancers and as such it represents a new target to circumvent chemotherapy resistance. In this chapter, we describe the screening test developed to identify molecules able to inhibit the drug efflux activity of Patched. This screening test uses yeast overexpressing functional human Patched that have been shown to resist to chemotherapeutic agents. This test can be adapted to other MDR transporters.
Insights
Researchers developed a screening test to find molecules that inhibit the multidrug resistance (MDR) transporter Patched, offering a new strategy against chemotherapy resistance in cancer.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Multidrug resistance (MDR) significantly reduces the effectiveness of anticancer drugs, hindering successful cancer chemotherapy.
- The Hedgehog receptor Patched acts as a multidrug transporter and is found in various cancers, presenting a potential target to overcome MDR.
Purpose of the Study:
- To describe a screening test designed to identify molecules that can inhibit the drug efflux activity of the Patched transporter.
- To provide a novel approach for developing new anticancer therapies that circumvent MDR.
Main Methods:
- Developed a screening test utilizing yeast engineered to overexpress functional human Patched.
- The yeast strains exhibit resistance to chemotherapeutic agents, serving as a model system.
Main Results:
- Successfully established a screening assay to identify inhibitors of Patched-mediated drug efflux.
- The developed test demonstrates potential for adaptation to screen for inhibitors of other MDR transporters.
Conclusions:
- The screening test offers a viable method for discovering novel compounds targeting Patched.
- This approach could lead to new therapeutic strategies to combat chemotherapy resistance in cancer patients.
