Cholesterol Regulation of Ion Channels and Receptors

This book brings together the most up–to–date knowledge about the role of cholesterol in regulation of ion channels and receptors and the pathological implications of these effects. It provides a comprehensive critical overview of the field comprised of three sections focusing on the impact of cholesterol on membrane structure, cholesterol regulation of ion channels and cholesterol regulation of receptors. This resource stands as a primary source of information for researchers both in academia and industrial drug development alike.

FOREWORD vii PREFACE ix CONTRIBUTORS xi I CHOLESTEROL REGULATION OF MEMBRANE PROPERTIES 1 1 CHOLESTEROL TRAFFICKING AND DISTRIBUTION BETWEEN CELLULAR MEMBRANES 3 Daniel Wu¨ stner, Lukasz Michael Solanko, and Frederik W. Lund 2 CHOLESTEROL REGULATION OF MEMBRANE PROTEIN FUNCTION BY CHANGES IN BILAYER PHYSICAL PROPERTIES—AN ENERGETIC PERSPECTIVE 27 Jens A. Lundbæk and Olaf S. Andersen II CHOLESTEROL REGULATION OF ION CHANNELS 45 3 INSIGHTS INTO STRUCTURAL DETERMINANTS OF CHOLESTEROL SENSITIVITY OF KIR CHANNELS 47 Avia Rosenhouse–Dantsker and Irena Levitan 4 ROLE OF LIPID RAFTS IN THE REGULATION OF STORE–OPERATED CA2+ CHANNELS 69 Hwei L. Ong and Indu S. Ambudkar 5 CHOLESTEROL REGULATION OF CARDIAC ION CHANNELS 91 Elise Balse, Ste´ phane Hatem, and Stanley Nattel 6 DIFFERENTIAL CONTRIBUTION OF BK SUBUNITS TO NONGENOMIC REGULATION OF CHANNEL FUNCTION BY STEROIDS 109 Alex M. Dopico, Anna N. Bukiya, and Aditya K. Singh 7 REGULATION OF K+ CHANNELS BY CHOLESTEROL–RICH MEMBRANE DOMAINS IN THE IMMUNE SYSTEM 135 Nu´ ria Comes and Antonio Felipe 8 INDIRECT CHANNEL REGULATION BY CHOLESTEROL: THE ROLE OF CAVEOLAE AND CAVEOLINS IN REGULATING KATP CHANNEL FUNCTION 161 Caroline Dart III CHOLESTEROL REGULATION OF RECEPTORS 181 9 REGULATION OF THE NICOTINIC ACETYLCHOLINE RECEPTOR BY CHOLESTEROL AS A BOUNDARY LIPID 183 Francisco J. Barrantes 10 SPECIFIC AND NONSPECIFIC REGULATION OF GPCR FUNCTION BY CHOLESTEROL 205 Gerald Gimpl and Katja Gehrig–Burger 11 STRUCTURAL INSIGHTS INTO CHOLESTEROL INTERACTIONS WITH G–PROTEIN–COUPLED RECEPTORS 231 Jeremiah S. Joseph, Enrique E. Abola, and Vadim Cherezov 12 MEMBRANE CHOLESTEROL: IMPLICATIONS IN RECEPTOR FUNCTION 255 Sandeep Shrivastava and Amitabha Chattopadhyay 13 THE ROLE OF CHOLESTEROL AND LIPID RAFTS IN REGULATION OF TLR RECEPTORS 273 Ruxana T. Sadikot INDEX 281