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Multidrug resistance transporters and modulation.
B Tan1, D Piwnica-Worms, L Ratner
1Department of Medicine, Washington University School of Medicine, St. Louis, Missouri, USA.
Current Opinion in Oncology
|September 7, 2000
Summary
Multidrug resistance (MDR) in cancer involves proteins like P-gp, MRP1, LRP, and BCRP that reduce drug effectiveness. New MDR inhibitors aim to overcome this resistance and improve cancer treatment outcomes.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Multidrug resistance (MDR) significantly limits cancer chemotherapy efficacy.
- Key MDR proteins include P-glycoprotein (P-gp), MRP1, LRP, and BCRP, which reduce intracellular drug accumulation.
- These proteins are linked to poor prognosis in various cancers, including AIDS-associated neoplasms.
Purpose of the Study:
- To review the molecular basis of MDR and the development of MDR-reversing agents.
- To discuss the limitations and potential applications of MDR modulators in cancer therapy.
Main Methods:
- Literature review of molecular investigations into MDR.
- Analysis of different generations of MDR inhibitors and their clinical development stages.
Main Results:
- Identification of specific MDR-associated proteins (P-gp, MRP1, LRP, BCRP).
- Development of first-, second-, and third-generation MDR inhibitors with varying efficacies and toxicities.
- Exploration of MDR modulators for enhancing drug delivery across biological barriers.
Conclusions:
- MDR remains a major challenge in cancer treatment.
- Ongoing research focuses on developing safer and more effective MDR inhibitors.
- MDR modulators show promise in improving drug penetration to sanctuary sites and enhancing absorption.