Abstract
P-glycoprotein (P-gp) is an ATP-driven transmembrane transporter capable of effluxing a wide variety of structurally diverse and functionally unrelated hydrophobic compounds out of the cell. Multidrug resistance (MDR), often associated with the over-expression of P-gp, has been implicated as a major obstacle to effective chemotherapy for cancer, parasitic diseases, AIDS, and other diseases. Drug efflux mediated by P-gp is also involved in decreasing the oral bioavailability of drugs by limiting intestinal absorption. Our appreciation of the structural and functional aspects of P-gp has definitely improved in recent years, benefiting from the deciphering of the structure of some bacterial transporters that paved the way for construction of homology models for more complex transporters. Here, we will review the recent advances in the studies of the structure and functional characteristics of P-gp with the hopes of facilitating rational drug design in developing novel potent MDR modulators.
Keywords: P-glycoprotein (P-gp), Structure, Function, MDR, Chemosensitizers
Current Medicinal Chemistry
Title: The Structure and Functions of P-Glycoprotein
Volume: 17 Issue: 8
Author(s): Y. Li, H. Yuan, K. Yang, W. Xu, W. Tang and X. Li
Affiliation:
Keywords: P-glycoprotein (P-gp), Structure, Function, MDR, Chemosensitizers
Abstract: P-glycoprotein (P-gp) is an ATP-driven transmembrane transporter capable of effluxing a wide variety of structurally diverse and functionally unrelated hydrophobic compounds out of the cell. Multidrug resistance (MDR), often associated with the over-expression of P-gp, has been implicated as a major obstacle to effective chemotherapy for cancer, parasitic diseases, AIDS, and other diseases. Drug efflux mediated by P-gp is also involved in decreasing the oral bioavailability of drugs by limiting intestinal absorption. Our appreciation of the structural and functional aspects of P-gp has definitely improved in recent years, benefiting from the deciphering of the structure of some bacterial transporters that paved the way for construction of homology models for more complex transporters. Here, we will review the recent advances in the studies of the structure and functional characteristics of P-gp with the hopes of facilitating rational drug design in developing novel potent MDR modulators.
Export Options
About this article
Cite this article as:
Li Y., Yuan H., Yang K., Xu W., Tang W. and Li X., The Structure and Functions of P-Glycoprotein, Current Medicinal Chemistry 2010; 17 (8) . https://dx.doi.org/10.2174/092986710790514507
DOI https://dx.doi.org/10.2174/092986710790514507 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
-
On the Role of Rab5 in Cell Migration
Current Molecular Medicine Antipsychotics as Psychosis Drugs and Neuroprotective Promoters Evaluated by Chemical QSAR - in silico and in vivo Studies
Letters in Drug Design & Discovery Eph Receptor Tyrosine Kinases in Tumor and Tumor Microenvironment
Current Pharmaceutical Design Potential Interactions between miRNAs and Hypoxia: A New Layer in Cancer Hypoxia
Anti-Cancer Agents in Medicinal Chemistry Some Implications of Receptor Kinase Signaling Pathway for Development of Multitargeted Kinase Inhibitors
Current Radiopharmaceuticals Anti-Amyloidogenic and Anti-Apoptotic Role of Melatonin in Alzheimer Disease
Current Neuropharmacology From Hybrids to New Scaffolds: The Latest Medicinal Chemistry Goals in Multi-target Directed Ligands for Alzheimer’s Disease
Current Neuropharmacology Current Prodrug Design for Drug Discovery
Current Pharmaceutical Design The Role of the PACAP Signaling System in Depression
Current Pharmaceutical Design Membrane Rafts in the Respiratory System
Current Respiratory Medicine Reviews Plant Defensins and Defensin-Like Peptides - Biological Activities and Biotechnological Applications
Current Pharmaceutical Design Targeting IGF-I, IGFBPs and IGF-I Receptor System in Cancer: The Current and Future in Breast Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery Regulation of Lactosylceramide Synthase (Glucosylceramide β1→4 Galactosyltransferase); Implication as A Drug Target
Current Drug Targets Small Molecule Toxins Targeting Tumor Receptors
Current Pharmaceutical Design Selective Toxicity of Apigenin on Cancerous Hepatocytes by Directly Targeting their Mitochondria
Anti-Cancer Agents in Medicinal Chemistry Human Platelets Express Authentic CB1 and CB2 Receptors
Current Neurovascular Research Targeted Angiogenesis Therapy in Head and Neck Squamous Cell Carcinomas
Current Angiogenesis (Discontinued) Meloxicam Prevents Load-Induced Cardiac Hypertrophy in Mice
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Towards Retinoid Therapy for Alzheimers Disease
Current Alzheimer Research Apoptosis-Inducing Activity of the S100A8/A9 Heterodimer
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry