1st Edition

Aquaporins in Health and Disease New Molecular Targets for Drug Discovery

Edited By Graca Soveral, Soren Nielsen, Angela Casini Copyright 2016
    356 Pages 16 Color & 47 B/W Illustrations
    by CRC Press

    356 Pages 16 Color & 47 B/W Illustrations
    by CRC Press

    356 Pages 16 Color & 47 B/W Illustrations
    by CRC Press

    Since the discovery of Aquaporin-1 (AQP1) as a water channel, many studies have revealed the importance of aquaporins in mammalian physiology and pathophysiology as well as plant and microbial biology. The studies have also shown aquaporins as potential drug targets and targets for improving crop properties.

    Written by an international group of contributors at the forefront of the field, Aquaporins in Health and Disease: New Molecular Targets for Drug Discovery presents the latest research advances in aquaporins and other major intrinsic protein (MIP) channels. The first section of the book describes the general concepts of aquaporin channel function, genomic research, structure-function analysis of aquaporins and glycerol facilitators, and regulation by gating and trafficking, including yeast aquaporin regulation and function. The second section discusses the physiological and pathophysiological roles of aquaporins in humans and microbes. The final section covers the development of inhibitors of aquaporin function. The book’s epilogue offers future perspectives and directions, mainly in the area of aquaporin-based diagnostics and therapeutics.

    Stimulating future research on this important protein family, this book facilitates a paradigm shift in the understanding and roles of aquaporin membrane proteins in all biological settings. It encourages scientists to develop novel approaches for the treatment of human diseases based on aquaporin function or dysfunction.

    Preface
    Søren Nielsen and Peter Agre

    MECHANISMS OF FLUID TRANSPORT IN CELLS AND EPITHELIA
    Aquaporin Functional Detection: Basic Concepts on Water and Solute Permeation
    Ana Madeira, Teresa F. Moura, and Graça Soveral
    Aquaporin Discovery in the Genomic Era
    Rafael Zardoya, Iker Irisarri, and Federico Abascal
    Aquaporin Structure and Selectivity
    Ardeschir Vahedi-Faridi and Andreas Engel
    Regulation of Eukaryotic Aquaporins
    Maria Nyblom and Susanna Törnroth-Horsefield
    Yeast Aquaporins and Aquaglyceroporins: A Matter of Lifestyle
    Mikael Andersson and Stefan Hohmann

    AQUAPORINS IN HEALTH AND DISEASE
    Aquaporins in Health
    Amaia Rodríguez, Leire Méndez-Giménez, and Gema Frühbeck
    Renal Aquaporins: Role in Water Balance Disorders
    Tae-Hwan Kwon and Søren Nielsen
    Vasopressin and the Regulation of Aquaporin-2 in Health and Disease
    Giovanna Valenti and Grazia Tamma
    Hepatobiliary, Salivary Glands and Pancreatic Aquaporins in Health and Disease
    Giuseppe Calamita, Christine Delporte, and Raúl A. Marinelli
    Aquaporins within the Central Nervous System: Implications for Oedema Following Traumatic CNS Injury
    Anna V. Leonard and Renée J. Turner
    Aquaporins in Carcinogenesis: Water and Glycerol Channels as New Potential Drug Targets
    Chulso Moon and David Moon
    Attacking Aquaporin Water and Solute Channels of Human-Pathogenic Parasites: New Routes for Treatment?
    Julia von Bülow and Eric Beitz

    AQUAPORINS AS DRUG TARGETS
    Aquaporins: Chemical Inhibition by Small Molecules
    Vincent J. Huber, Sören Wacker, and Michael Rützler
    Drug Discovery and Therapeutic Targets for Pharmacological Modulators of Aquaporin Channels
    Jinxin V. Pei, Joshua L. Ameliorate, Mohamad Kourghi, Michael L. De Ieso, and Andrea J. Yool
    Inorganic Compounds as Aquaporin Substrates or as Potent Inhibitors: A Coordination Chemistry Point of View
    Angela Casini and Andreia de Almeida

    Epilogue
    Angela Casini and Graça Soveral

    Biography

    Graça Soveral is an associate professor in the Pharmacy School at the University of Lisbon and principal investigator at the Research Institute for Medicines (iMed.ULisboa), where she coordinates the Biological Transport Unit. She received a PhD in pharmacy, sub-area biochemistry, from the University of Lisbon. Her main research area is membrane transport, with a special emphasis on water and solute transport in cell physiology and osmoregulation, aquaporin gating, and the discovery of aquaporin modulators for diagnostic and therapeutic applications.

    Søren Nielsen is a professor in the Department of Health Science and Technology at Aalborg University. He received an MD and a dr.med.sci degree in medical sciences from Aarhus University. His research involves the cell and molecular biological, physiological, and pathophysiological studies of aquaporin membrane water channels (aquaporins), sodium channels, and transporters in kidney and other organs to explore their role in water and sodium balance regulation in health and disease.

    Angela Casini is the chair of medicinal and bioinorganic chemistry in the School of Chemistry at Cardiff University. She received a PhD in chemistry from the University of Florence. Her work in medicinal and bioinorganic chemistry focuses on the study of the molecular mechanisms of anticancer metallodrugs and the development of metal compounds as chemical probes to detect protein functions.

    Peter Agre co-authored the preface of this book. He is a professor and director of the Johns Hopkins Malaria Research Institute at Johns Hopkins University. He received an MD from Johns Hopkins University Medical School. Dr. Agre was awarded the 2003 Nobel Prize in Chemistry for his pioneering studies on aquaporins.