Abstract
Multidrug resistance (MDR) against groups of therapeutic drugs emerged to a central problem in the treatment of various diseases, i.e. cancer and infectious diseases like HIV or malaria. ABC transporters namely P-glycoprotein (P-gp) and various multidrug resistance associated proteins (MRPs) mainly contribute to the MDR phenomenon in cancer treatment and HIV therapy. Their cellular expression in respective cells like cancer cells lowers the intracellular drug concentrations and thus reasons the cellular resistance. The induction of such efflux pumps occurs during the therapy with drugs which will be affected by the MDR phenomenon as a consequence of the induction. In this review studies which report such drugs-caused inductions will be viewed. The review will cover the literature of recent years and attract attention to this important question in drug resistance. Finally, the discussion will suggest possible strategies to overcome the problem, i. e. by using non-inducing drugs.
Keywords: Drug therapy, efflux pumps, multidrug resistance, MDR modulators, transporter induction studies, transporter substrates, HIV-1 protease inhibitors, ABCB1, tipranavir
Mini-Reviews in Medicinal Chemistry
Title:The Impact of the Induction of Multidrug Resistance Transporters in Therapies by Used Drugs: Recent Studies
Volume: 12 Issue: 11
Author(s): A. Hilgeroth, M. Hemmer and C. Coburger
Affiliation:
Keywords: Drug therapy, efflux pumps, multidrug resistance, MDR modulators, transporter induction studies, transporter substrates, HIV-1 protease inhibitors, ABCB1, tipranavir
Abstract: Multidrug resistance (MDR) against groups of therapeutic drugs emerged to a central problem in the treatment of various diseases, i.e. cancer and infectious diseases like HIV or malaria. ABC transporters namely P-glycoprotein (P-gp) and various multidrug resistance associated proteins (MRPs) mainly contribute to the MDR phenomenon in cancer treatment and HIV therapy. Their cellular expression in respective cells like cancer cells lowers the intracellular drug concentrations and thus reasons the cellular resistance. The induction of such efflux pumps occurs during the therapy with drugs which will be affected by the MDR phenomenon as a consequence of the induction. In this review studies which report such drugs-caused inductions will be viewed. The review will cover the literature of recent years and attract attention to this important question in drug resistance. Finally, the discussion will suggest possible strategies to overcome the problem, i. e. by using non-inducing drugs.
Export Options
About this article
Cite this article as:
Hilgeroth A., Hemmer M. and Coburger C., The Impact of the Induction of Multidrug Resistance Transporters in Therapies by Used Drugs: Recent Studies, Mini-Reviews in Medicinal Chemistry 2012; 12 (11) . https://dx.doi.org/10.2174/138955712802762130
DOI https://dx.doi.org/10.2174/138955712802762130 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
Addressing the Challenge: Current and Future Directions in Ovarian Cancer Therapy
Current Gene Therapy Melatonin and Aromatase in Breast Cancer
Clinical Cancer Drugs 89Zr Radiochemistry for Positron Emission Tomography
Medicinal Chemistry Studies on Chloride Channels and their Modulators
Current Topics in Medicinal Chemistry Structure-based Virtual Screening Approaches in Kinase-directed Drug Discovery
Current Topics in Medicinal Chemistry Open Access High Throughput Drug Discovery in the Public Domain: A Mount Everest in the Making
Current Pharmaceutical Biotechnology SUBJECT INDEX TO VOLUME 4 Current Organic Chemistry
Current Organic Chemistry 3D-QSAR and Docking Simulation Studies of Some Benzopyrone Derivatives as Inhibitors for Breast Cancer Stem Cell Growth via PGlycoprotein Mediated Efflux
Current Bioinformatics RAS/RAF/MEK Inhibitors in Oncology
Current Medicinal Chemistry Privileged 1,2,4-Oxadiazoles in Anticancer Drug Design: Novel 5- Aryloxymethyl-1,2,4-oxadiazole Leads for Prostate Cancer Therapy
Letters in Drug Design & Discovery The Role of Mammalian Target of Rapamycin (mTOR) Inhibitors in the Treatment of Solid Tumors
Current Cancer Therapy Reviews Incidental Extracardiac Findings on Coronary Computed Tomography Angiography: A Pictorial Review of Imaging Findings
Current Medical Imaging Interplay of Drug Metabolizing CYP450 Enzymes and ABC Transporters in the Blood-Brain Barrier
Current Drug Metabolism Surface Markers of Cancer Stem Cells in Solid Tumors
Current Stem Cell Research & Therapy A Role for Tumor Suppressor Protein p53 in the Fidelity of DNA Synthesis and Resistance Towards Nucleoside Analogs
Current Cancer Therapy Reviews A Hidden Human Proteome Signature Characterizes the Epithelial Mesenchymal Transition Program
Current Pharmaceutical Design Molecular Signals Elicited by GPCR Agonists in Hypertension, Cardiovascular Remodeling: Are MMPs and ADAMs Elusive Therapeutic Targets?
Current Hypertension Reviews Revolutionary Impact of Nanodrug Delivery on Neuroscience
Current Neuropharmacology Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes
Current Medicinal Chemistry Multi-Target Profile of Oleocanthal, An Extra-Virgin Olive Oil Component
Current Bioactive Compounds