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Published on: June 25, 2017
Recent Progress in the Development of Glucose Transporter (GLUT) Inhibitors
Yuxuan Wang1, Zhiqiang Sun2, Zean Zhao2
1Zhujiang Hospital, The Second School of Clinical Medicine, Southern Medical University, Guangzhou 510280, China.
Abstract:
Cancer cells exhibit an accelerated glucose uptake and glycolysis. The transmembrane uptake of glucose requires specific carrier proteins, such as glucose transporters (GLUTs) and sodium-coupled glucose cotransporters (SGLTs). GLUTs transport glucose independently of the energy supply and have become promising targets for cancer therapy. This Perspective mainly focuses on the current research progress and design strategy of GLUT inhibitors, particularly those targeting class I (GLUT1-4). To the best of our knowledge, this is the first systematic interpretation of the research progress, opportunities, and challenges faced in the development of GLUT inhibitors from a medicinal chemistry perspective. We hope that this Perspective will provide insights into the development of GLUT inhibitors, offering a feasible approach to cancer therapy.
Insights
Cancer cells rely on glucose, using glucose transporters (GLUTs) for uptake. Inhibiting GLUTs offers a promising strategy for developing novel cancer therapies.
Area of Science:
- Biochemistry
- Oncology
- Medicinal Chemistry
Background:
- Cancer cells demonstrate increased glucose metabolism (glycolysis) and uptake.
- Glucose transport across cell membranes is facilitated by glucose transporters (GLUTs) and sodium-coupled glucose cotransporters (SGLTs).
- GLUTs are crucial for cancer cell survival and proliferation, making them attractive therapeutic targets.
Purpose of the Study:
- To provide a comprehensive overview of the research progress in developing GLUT inhibitors.
- To discuss the design strategies for GLUT inhibitors, focusing on class I GLUTs (GLUT1-4).
- To highlight the opportunities and challenges in GLUT inhibitor development for cancer therapy.
Main Methods:
- Systematic review of current research on GLUT inhibitors.
- Analysis of medicinal chemistry approaches for designing GLUT inhibitors.
- Focus on inhibitors targeting class I GLUTs (GLUT1-4).
Main Results:
- GLUT inhibitors represent a promising avenue for cancer treatment.
- Medicinal chemistry offers strategies for designing effective GLUT inhibitors.
- Significant progress has been made, but challenges remain in clinical translation.
Conclusions:
- Targeting GLUTs, particularly class I members, is a viable strategy for cancer therapy.
- Further research in medicinal chemistry is essential to overcome challenges and optimize GLUT inhibitor development.
- This perspective offers insights for advancing GLUT inhibitor-based cancer treatments.
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