Abstract
Modulators and inhibitors of multidrug efflux transporters, like P-glycoprotein, are used to reduce or inhibit multidrug resistance, MDR, which leads to a failure of the chemotherapy of e.g. cancers, epilepsy, bacterial, parasitic, and fungal diseases. Binding and transport of first-, second-, and third-generation modulators and inhibitors of P-glycoprotein are discussed, taking into account the properties of the drug (Hbonding potential, dimensions, and pKα values) as well as the properties of the membrane.
Keywords: p-glycoprotein, first, second, and third-generation inhibitors, modulators, membrane partitioning, transporter binding, transport kinetics
Mini-Reviews in Medicinal Chemistry
Title: Inhibitors of Multidrug Efflux Transporters: Their Membrane and Protein Interactions
Volume: 5 Issue: 2
Author(s): A. Seelig and E. Gatlik-Landwojtowicz
Affiliation:
Keywords: p-glycoprotein, first, second, and third-generation inhibitors, modulators, membrane partitioning, transporter binding, transport kinetics
Abstract: Modulators and inhibitors of multidrug efflux transporters, like P-glycoprotein, are used to reduce or inhibit multidrug resistance, MDR, which leads to a failure of the chemotherapy of e.g. cancers, epilepsy, bacterial, parasitic, and fungal diseases. Binding and transport of first-, second-, and third-generation modulators and inhibitors of P-glycoprotein are discussed, taking into account the properties of the drug (Hbonding potential, dimensions, and pKα values) as well as the properties of the membrane.
Export Options
About this article
Cite this article as:
Seelig A. and Gatlik-Landwojtowicz E., Inhibitors of Multidrug Efflux Transporters: Their Membrane and Protein Interactions, Mini-Reviews in Medicinal Chemistry 2005; 5 (2) . https://dx.doi.org/10.2174/1389557053402693
DOI https://dx.doi.org/10.2174/1389557053402693 |
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
-
Anticonvulsant and Neurological Profile of Benzothiazoles: A Mini-Review
Central Nervous System Agents in Medicinal Chemistry The Role of Microglial Cells on Neuroinflammation: Possible Therapeutic Applications
Recent Patents on Regenerative Medicine Natural Products as Modulators of Spermatogenesis: The Search for a Male Contraceptive
Current Molecular Pharmacology Synthesis and Screening of Substituted Thiosemicarbazone Derivatives: An Approach towards Novel Anticonvulsant Search
Central Nervous System Agents in Medicinal Chemistry N-3 (Omega-3) Polyunsaturated Fatty Acids in the Pathophysiology and Treatment of Depression: Pre-Clinical Evidence
CNS & Neurological Disorders - Drug Targets A New Interpretative Paradigm for Conformational Protein Diseases
Current Protein & Peptide Science From Surface to Nuclear Receptors: The Endocannabinoid Family Extends its Assets
Current Medicinal Chemistry Editorial [Hot Topic: Functions and Metabolism of Brain Nucleosides and their Metabolites (Guest Editors: Zsolt Kovacs & Arpad Dobolyi)]
Current Topics in Medicinal Chemistry Therapeutic Hypothermia as a Neuroprotective Strategy in Neonatal Hypoxic-Ischemic Brain Injury and Traumatic Brain Injury
Current Molecular Medicine GABAergic Agonists Modulate the Glutamate Release from Frontal Cortex Synaptosomes of Rats with Experimental Autoimmune Encephalomyelitis
Inflammation & Allergy - Drug Targets (Discontinued) Melatonin-mitochondria Interplay in Health and Disease
Current Topics in Medicinal Chemistry The Therapeutic Role of Electroencephalography in Deep Brain Stimulation in Intractable Epilepsy: A Recent Perspective
Recent Patents and Topics on Imaging (Discontinued) subject Index To Volume 2
Current Genomics Histamine H4 Receptor: A Novel Target for Inflammation Therapy
Mini-Reviews in Medicinal Chemistry Therapeutic Potential of Metabotropic GABA (GABAB) Receptors and their Effector Ion Channels
Central Nervous System Agents in Medicinal Chemistry Neurotransmitters and Chemokines Regulate Tumor Cell Migration: Potential for a New Pharmacological Approach to Inhibit Invasion and Metastasis Development
Current Pharmaceutical Design UCLA’s Molecular Screening Shared Resource: Enhancing Small Molecule Discovery with Functional Genomics and New Technology
Combinatorial Chemistry & High Throughput Screening Neuroimmune Crosstalk in CNS Disorders: The Histamine Connection
Current Pharmaceutical Design Anxiety: A Systematic Review of Neurobiology, Traditional Pharmaceuticals and Novel Alternatives from Medicinal Plants
CNS & Neurological Disorders - Drug Targets Bhasma: Indian Perspective of Nanomedicinal Technology
Recent Patents on Nanomedicine