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.

An essential text, this is a fully updated second edition of a classic, now in two volumes. It provides rapid access to information on molecular pharmacology for research scientists, clinicians and advanced students. With the A-Z format of over 2,000 entries, around 350 authors provide a complete reference to the area of molecular pharmacology. The book combines the knowledge of classic pharmacology with the more recent approach of the precise analysis of the molecular mechanisms by which drugs exert their effects. Short keyword entries define common acronyms, terms and phrases. In addition, detailed essays provide in-depth information on drugs, cellular processes, molecular targets, techniques, molecular mechanisms, and general principles.

This book is devoted to the fascinating superfamily of plant ATP-binding cassette (ABC) transporters and their variety of transported substrates. It highlights their exciting biological functions, covering aspects ranging from cellular detoxification, through development, to symbiosis and defense. Moreover, it also includes a number of chapters that center on ABC transporters from non-Arabidopsis species. ABC proteins are ubiquitous, membrane-intrinsic transporters that catalyze the primary (ATP-dependent) movement of their substrates through biological membranes. Initially identified as an essential aspect of a vacuolar detoxification process, genetic work in the last decade has revealed an unexpectedly diverse variety of ABC transporter substrates, which include not only xenobiotic conjugates, but also heavy metals, lipids, terpenoids, lignols, alkaloids and organic acids. The discovery that members of the ABCB and ABCG family are involved in the movement of phytohormones has further sparked their exploration and provided a new understanding of the whole family. Accordingly, the trafficking, regulation and structure-function of ABCB-type auxin transporters are especially emphasized in this book.

This book provides with a comprehensive overview of the role of drug transporters in drug disposition and efficacy/toxicity, as well as drug-drug interactions and recent advances in the field. Transporters are known determinants of drug disposition and efficacy/toxicity. In general, they are divided into solute carrier (SLC) and ATP binding cassette (ABC) families, and are located along cell membranes, where they mediate drug uptake into cells and export out of cells. Drug transporters are essential in maintaining cell homeostasis, and their gene mutations may cause or contribute to severe human genetic disorders, such as cystic fibrosis, neurological disease, retinal degeneration, anemia, and cholesterol and bile transport defects. Conversely, some diseases may also alter transporter functions and expressions, in turn aggravating disease process. Further, since over-expression of some ABC transporters is a potential contributor to multidrug-resistance (MDR), the book presents a number of strategies to overcome MDR, including ABC transporter inhibitors and applying epigenetic methods to modulate transporter expressions and functions. This book is useful for graduate students and professionals who are looking to refresh or expand their knowledge of this exciting field.

This book, written by leading international experts, provides a comprehensive, current examination of transport-mediated antimicrobial resistance. As a particularly powerful mechanism of multidrug resistance, an in-depth examination of efflux pumps is conducted with bacteria of major public health concern including Enterobacteriaceae, Acinetobacter, Neisseria, Pseudomonas, staphylococci, and mycobacteria. The content spans structural biochemistry and transport mechanisms of the major transporter families and considers individual drug efflux systems across various Gram-positive and Gram-negative species. Genomic analysis of efflux pump distribution and their contribution to clinically-relevant resistance are a major focus of the text. Moreover, interplay between drug efflux pumps and other key resistance mechanisms such as intrinsic drug impermeability, inactivation, and target alterations are discussed, as well as their molecular expression-based regulation and physiological functions beyond resistance, involving biofilms, stress response, and pathogenicity. Finally, strategies are addressed to target this drug resistance mechanism with novel antimicrobials or drug inhibitor adjuvants.

Ocular transporters and receptors contains detailed descriptions of major transporters and receptors expressed in the eye, with special emphasis on their role in drug delivery. The complex anatomy and the existence of multiple barriers in the eye pose a considerable challenge to successful drug delivery to the eye. Hence ocular transporters and receptors are important targets for drug delivery. A significant advancement has been made in the field of ocular transport research and their role in drug delivery. In this book the cutting edge research being carried out in this field is compiled and summarized. The book focuses on key areas, including the anatomy and physiology of the eye, biology of ocular transporters and receptors, techniques in characterization of transporters and receptors, transporters and receptors in the anterior and posterior segment in the eye, the role of ocular transporters and receptors in drug delivery, and transporter-metabolism interplay in the eye. - Highly focused on ocular transporters - Most up-to-date research compilation - Detailed description of role of transporters and receptors in ocular drug discovery and delivery