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Printed Glycan Array: A Sensitive Technique for the Analysis of the Repertoire of Circulating Anti-carbohydrate Antibodies in Small Animals
Published on: February 14, 2019
Recent advances in the research of P-glycoprotein inhibitors
Kanghui Yang1, Jifeng Wu, Xun Li
1Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province, China.
Abstract:
The ability of cancer cells to experience intrinsic or acquired resistance to a broad spectrum of structurally and functionally unrelated chemotherapeutic agents, termed multidrug resistance (MDR), is the most common cause of chemotherapy failure. Research has firmly established that most tumors developing MDR are often associated with the over-expression of permeability-glycoprotein (P-gp), the most extensively characterized of the drug efflux pumps. The development of P-gp inhibitors is acknowledged as a viable means of reversing this MDR phenotype and has received considerable attention throughout the past two decades. However, most P-gp inhibitors identified to date have demonstrated limited clinical success due to limitations in potency and specificity. This paper reviews the most recent discoveries relating to the medicinal chemistry of P-gp inhibitors that are presently in development. In light of this information, this paper seeks to suggest new treatment options for the MDR phenotype.
Insights
Multidrug resistance (MDR) in cancer is often caused by drug efflux pumps like P-glycoprotein (P-gp). This review explores new P-gp inhibitors to overcome chemotherapy failure and suggest novel treatment options.
Area of Science:
- Oncology
- Pharmacology
- Medicinal Chemistry
Background:
- Multidrug resistance (MDR) is a major cause of chemotherapy failure in cancer treatment.
- Over-expression of P-glycoprotein (P-gp), a drug efflux pump, is strongly linked to MDR development in tumors.
- Current P-gp inhibitors show limited clinical success due to insufficient potency and specificity.
Purpose of the Study:
- To review recent advancements in the medicinal chemistry of P-glycoprotein (P-gp) inhibitors.
- To identify potential new therapeutic strategies for overcoming the multidrug resistance (MDR) phenotype.
Main Methods:
- Literature review of recent discoveries in P-gp inhibitor development.
- Analysis of medicinal chemistry approaches targeting P-gp.
Main Results:
- Identification of novel P-gp inhibitors currently in development.
- Evaluation of their potency and specificity compared to existing agents.
Conclusions:
- Despite challenges, ongoing research in P-gp inhibitor medicinal chemistry offers promise for reversing MDR.
- Newer inhibitors may provide improved efficacy and specificity, leading to better cancer treatment outcomes.
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