Abstract
Increased glycolysis has been one of the metabolic characteristics known as the Warburg effect. The functional and therapeutic importance of the Warburg effect in targeted therapy is scientifically recognized and the glucose metabolic pathway has become a desirable target of anticancer strategies. Glucose transporters (GLUTs) play an important role in cancer glycolysis to sustain cancer cell proliferation, metastasis and survival. Utilizing the knowledge of differential expression and biological functions of GLUTs offers us the possibility of designing and delivering chemotherapeutics toward targeted tumor tissues for improved cancer selectivity. Inhibition of glucose uptake or glycolysis may effectively kill hypoxic cancer cells. Facilitative drug uptake via active transportation provides the potential opportunity to circumvent the drug resistance in chemotherapy. GLUTs as the hallmarks and biotargets of cancer metabolism enable the design and development of novel targeted theranostic agents. In this updated review, we examine the current scenario of the GLUTs as strategic targets in cancer and the unique concepts for discovery and development of GLUTs-targeted anticancer agents. We highlight the recent progresses on structural biology and underlying mechanism studies of GLUTs, with a brief introduction to the computational approaches in GLUT-mediated drug transport and tumor targeting.
Keywords: Glucose transporters, Warburg effect, Drug design, Transport mechanism, Structural biology, Targeted therapy, Medicinal chemistry.
Current Topics in Medicinal Chemistry
Title:Targeting Key Transporters in Tumor Glycolysis as a Novel Anticancer Strategy
Volume: 18 Issue: 6
Author(s): Yunli Shi, Shengnan Liu, Shabir Ahmad and Qingzhi Gao*
Affiliation:
- Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, Collaborative Innovation Center of Chemical Science and Engineering, School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Nankai District, Tianjin 300072,China
Keywords: Glucose transporters, Warburg effect, Drug design, Transport mechanism, Structural biology, Targeted therapy, Medicinal chemistry.
Abstract: Increased glycolysis has been one of the metabolic characteristics known as the Warburg effect. The functional and therapeutic importance of the Warburg effect in targeted therapy is scientifically recognized and the glucose metabolic pathway has become a desirable target of anticancer strategies. Glucose transporters (GLUTs) play an important role in cancer glycolysis to sustain cancer cell proliferation, metastasis and survival. Utilizing the knowledge of differential expression and biological functions of GLUTs offers us the possibility of designing and delivering chemotherapeutics toward targeted tumor tissues for improved cancer selectivity. Inhibition of glucose uptake or glycolysis may effectively kill hypoxic cancer cells. Facilitative drug uptake via active transportation provides the potential opportunity to circumvent the drug resistance in chemotherapy. GLUTs as the hallmarks and biotargets of cancer metabolism enable the design and development of novel targeted theranostic agents. In this updated review, we examine the current scenario of the GLUTs as strategic targets in cancer and the unique concepts for discovery and development of GLUTs-targeted anticancer agents. We highlight the recent progresses on structural biology and underlying mechanism studies of GLUTs, with a brief introduction to the computational approaches in GLUT-mediated drug transport and tumor targeting.
Export Options
About this article
Cite this article as:
Shi Yunli , Liu Shengnan , Ahmad Shabir and Gao Qingzhi *, Targeting Key Transporters in Tumor Glycolysis as a Novel Anticancer Strategy, Current Topics in Medicinal Chemistry 2018; 18 (6) . https://dx.doi.org/10.2174/1568026618666180523105234
DOI https://dx.doi.org/10.2174/1568026618666180523105234 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Chronic Kidney Disease
The scope of the special thematic issue includes but not limited to the mechanism of chronic kidney disease (CKD), the treatment of renal fibrosis and early diagnosis of CKD and so on. We also welcome manuscripts from other scientific research area with respect to internal medicine. Cell death has been ...read more
![](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Drug Repurposing in the Development of Anticancer Agents
Current Medicinal Chemistry The Immunological Side-Effects of Sedative Agents in the Intensive Care Unit
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Targeting the Akt/PI3K Signaling Pathway as a Potential Therapeutic Strategy for the Treatment of Pancreatic Cancer
Current Medicinal Chemistry Reconceptualizing Adult Neurogenesis: Role for Sphingosine-1-Phosphate and Fibroblast Growth Factor-1 in Co-Ordinating Astrocyte-Neuronal Precursor Interactions
CNS & Neurological Disorders - Drug Targets Quinolone Derivatives as Anticancer Agents: Importance in Medicinal Chemistry
Current Topics in Medicinal Chemistry Insulin-Like Growth Factor 2 - The Oncogene and its Accomplices
Current Pharmaceutical Design Clinically Relevant Genetic Variations in Drug Metabolizing Enzymes
Current Drug Metabolism Signal Transduction of Steroidogenic Hormones to the Adrenal and Gonadal Mitochondria and the Possibilities for Combating Lipoid Congenital Adrenal Hyperplasia
Current Signal Transduction Therapy Current Research on Opioid Receptor Function
Current Drug Targets An “Enigmatic” L-Carnosine (β-Alanyl-L-Histidine)? Cell Proliferative Activity as a Fundamental Property of a Natural Dipeptide Inherent to Traditional Antioxidant, Anti-Aging Biological Activities: Balancing and a Hormonally Correct Agent, Novel Patented Oral Therapy Dosage Formulation for Mobility, Skeletal Muscle Power and Functional Performance, Hypothalamic-Pituitary- Brain Relationship in Health, Aging and Stress Studies
Recent Patents on Drug Delivery & Formulation Physiology and Pharmacology of Two-Pore Domain Potassium Channels
Current Pharmaceutical Design Antitumor Carbazoles
Anti-Cancer Agents in Medicinal Chemistry Effects of Exercise on Anxiety and Depression Disorders: Review of Meta- Analyses and Neurobiological Mechanisms
CNS & Neurological Disorders - Drug Targets Chemokines as Therapeutic Targets in Non-Small Cell Lung Cancer
Current Medicinal Chemistry - Anti-Cancer Agents Genetics, Structure, Function, Mode of Actions and Role in Cancer Development of CYP17
Anti-Cancer Agents in Medicinal Chemistry Discovery of Polo-like Kinase 4 Inhibitors for the Treatment of Cancer: A Mini Patent Review
Mini-Reviews in Medicinal Chemistry The Regulation of Neuroimmune-Endocrine Interactions: Mechanisms,Molecular Pathways Unraveled and the Pivotal Role of Cytokines – A Unsung Putative Bidirectional Interdependence between the Immune and Neuroendocrine Interfaces
Current Immunology Reviews (Discontinued) Radiopharmaceuticals to In Vivo Characterize Adrenal Incidentalomas:The Integrated Role of Radionuclide and Radiological Techniques
Current Radiopharmaceuticals An Insight into Drug Repositioning for the Development of Novel Anti-Cancer Drugs
Current Topics in Medicinal Chemistry Identification of AHSA1 as a Potential Therapeutic Target for Breast Cancer: Bioinformatics Analysis and <i>in vitro</i> Studies
Current Cancer Drug Targets