Membrane Transporters and Channels as Targets for Drugs

Membrane Transporters and Channels as Targets for Drugs

Author: Graça Soveral

Publisher: Frontiers Media SA

Published: 2020-01-03

Total Pages: 333

ISBN-13: 2889633578

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Transporters and channels are membrane proteins that mediate the traffic of metabolites, water and ions across biological membranes. Membrane transport proteins are crucial to maintain homeostasis and assure cell survival upon intracellular or environmental stress. A failure of any of these transport systems may have dramatic consequences for cell function. There is increasing evidence that membrane transport proteins play important functions in healthy conditions and that their absence or dysfunction may cause diseases. In recent years much attention has been paid to diseases resulting from defective transporters (“carrier diseases”) and ion channels (“channelopathies”). Very interestingly, altered expression of transporters has been described in several human pathologies. On this basis, many transport proteins are well acknowledged targets for drugs. Many others are involved in drug delivery and disposition and/or are considered potential targets. Others are off-targets for drugs and then, are responsible for side effects. Thus, membrane protein drug discovery is now an emerging field where the search for physiological mechanisms of regulation and for chemical compounds as modulators of transport activity, present new opportunities for drug development and for new therapies. This Research Topic addresses the latest research advances in membrane transport proteins, stimulating future research on these important protein families.


Membrane Transporters as Drug Targets

Membrane Transporters as Drug Targets

Author: Gordon L. Amidon

Publisher: Springer Science & Business Media

Published: 2006-04-11

Total Pages: 547

ISBN-13: 0306468123

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Because progress in the field of transporters has been extraordinary, this volume will focus on recent advances in our understanding of the structure, function, physiology, and molecular biology of membrane transporters. There will be an emphasis on transporters as molecular targets for drug delivery and disposition in the body.


Transporters as Drug Targets

Transporters as Drug Targets

Author: Gerhard F. Ecker

Publisher: John Wiley & Sons

Published: 2017-04-10

Total Pages: 354

ISBN-13: 3527333843

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As opposed to other books on the topic, this volume is unique in also covering emerging transporter targets. Following a general introduction to the importance of targeting transporter proteins with drugs, the book systematically presents individual transporter classes and explains their pharmacology and physiology. The text covers all transporter families with known or suspected importance as drug targets, including neurotransmitter transporters, ABC transporters, glucose transporters and organic ion transporters. The final part discusses recent advances in structural studies of transport proteins, assay methods for transport activity, and the systems biology of transporters and their regulation. With its focus on drug development issues, this authoritative overview is required reading for researchers in industry and academia targeting transport proteins for the treatment of disease.


Membrane Transporters in Drug Discovery and Development

Membrane Transporters in Drug Discovery and Development

Author: Qing Yan

Publisher: Methods in Molecular Biology

Published: 2010-04-26

Total Pages: 390

ISBN-13:

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This text provides practical methodologies of the ongoing research on membrane transporters, considering applications of transporter technologies in drug discovery and development.


Drug Transporters

Drug Transporters

Author: Guofeng You

Publisher: John Wiley & Sons

Published: 2022-04-06

Total Pages: 1269

ISBN-13: 111973987X

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DRUG TRANSPORTERS Drug transporter fundamentals and relevant principles and techniques, featuring new and expanded chapters Drug Transporters: Molecular Characterization and Role in Drug Disposition provides in-depth analysis of the conceptual evolution and technical development for studying drug transporters. Contributions by an international panel of leading researchers address advances in transporters as drug targets, transporters in pharmacotherapy, the impact of transporters on drug efficacy and safety, the development of sophisticated model systems and sensitive assay methods, and more. Divided into two parts, the book first provides a thorough overview of relevant drug transporters before detailing the principles of drug transport and associated techniques. The updated and expanded third edition includes new chapters on in vitro-in vivo scale-up of drug transport activities, the ontogeny of drug transporters, the application of physiologically-based pharmacokinetic and pharmacodynamic modeling, and the use of transporters as therapeutic targets for diseases. Reflects the current state of the field and offers perspectives on future directions Covers basic knowledge, clinical outcomes, and emerging discoveries in transporter science Provides up-to-date information on drug transporter families, mechanisms, and clinical implications Includes extensive references and numerous figures and tables throughout Understandable for novices while offering sufficient depth for more experienced researchers, Drug Transporters: Molecular Characterization and Role in Drug Disposition, Third Edition is an excellent textbook for pharmacological or physiological science courses in drug/membrane transport, and an invaluable reference for academic or industrial scientists working in the transporter field and related areas of drug metabolism, pharmacokinetics, and pharmacodynamics.


Drug Transporters

Drug Transporters

Author: Martin F. Fromm

Publisher: Springer Science & Business Media

Published: 2010-11-19

Total Pages: 457

ISBN-13: 3642145418

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It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.


Transporters in Drug Discovery and Development

Transporters in Drug Discovery and Development

Author: Yurong Lai

Publisher: Woodhead Publishing

Published: 2014-08-22

Total Pages: 759

ISBN-13: 190881828X

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Written by a leading researcher in the field, Transporters in Drug Discovery and Development provides a comprehensive and practical guide to drug transporter families that are the most important for drug discovery and development. It covers: an overview of transporter families and organ distribution; clinical relevant drug-drug interaction; clinical relevant polymorphism; drug transporter related pharmacokinetic, pharmacodynamics and toxicity; in vitro/in vivo probes of drug transport studies; the practical methodologies of industrial transporter screening and translational aspect in drug discovery and developments. A comprehensive overview of drug transporter families and their clinical relevance in drug discovery and development Balanced coverage of molecular biology aspects and functional outcomes State of art knowledge related to transporter-mediated DDI and the clinical relevance in pharmacokinetics, dynamics, and toxicity


Membrane Transporters

Membrane Transporters

Author: Qing Yan

Publisher: Springer Science & Business Media

Published: 2008-02-02

Total Pages: 374

ISBN-13: 1592593879

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Studies of membrane transporters have had great impact on our und- standing human diseases and the design of effective drugs. About 30% of current clinically marketed drugs are targeting membrane transporters or channels. Membrane Transporters: Methods and Protocols provides various practical methodologies for the ongoing research on membrane transporters. To provide readers the most up-to-date information, several emerging fields and methodologies are embraced in this book, including pharmacogenomics, bioin-formatics, and microarray technology. Pharmacogenomics studies of membrane transporters are useful in drug discovery and in predicting drug responses in the clinic. In this volume, the current status of pharma- genomics studies of transporters is reviewed and research methodologies in this field are described. Transporter classification is important in studying the structure and function of membrane transporters and has thus triggered intensive interest in recent years. Membrane Transporters: Methods and Protocols provides a systematic classification of all transmembrane transport proteins found in living org- isms on Earth. This classification system will be helpful for further studies on various aspects of membrane transporters, especially for such large-scale gene expression studies as those employing microarray technologies. Bioinformatics is frequently used in transporter studies and has become indispensable for all kinds of research methods. Commonly used bio- formatics methods, such as databases and tools for sequence analysis and - tif studies, are explained in order to facilitate membrane transporters research. Because of heterogeneous sources and tremendous amounts of data, data in- gration has become one of the most important issues in transporter studies.


Transporters in Drug Development

Transporters in Drug Development

Author: Yuichi Sugiyama

Publisher: Springer Science & Business Media

Published: 2013-09-16

Total Pages: 322

ISBN-13: 1461482291

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Transporters in Drug Development examines how membrane transporters can be dealt with in academic–industrial drug discovery and pharmaceutical development as well as from a regulatory perspective. The book describes methods and examples of in vitro characterization of single transporters in the intestines, liver and kidneys as well as characterization of substrate overlap between various transporters. Furthermore, probes and biomarkers are suggested for studies of the transporters’ impact on the pharmacokinetics of drug substrates/candidates interacting on transporters. The challenges of translating in vitro observed interaction of transporters into in vivo relevance are explored, and the book highlights perspectives of applying targeted proteomics and mechanistic modeling in this process.