Molecular Biology in Medicinal Chemistry - Steinhilber.pdf

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Molecular Biology in
Medicinal Chemistry
Edited by Th. Dingermann,
D. Steinhilber and
G. Folkers
Molecular Biology in Medicinal Chemistry. Edited by Th. Dingermann, D. Steinhilber, G. Folkers
Copyright
2004 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
ISBN: 3-527-30431-2
8
Methods and Principles in
Medicinal Chemistry
Edited by R. Mannhold, H. Kubinyi,
G. Folkers
oltje, H. Timmerman, J. Vacca,
H. van de Waterbeemd, T. Wieland
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Editorial Board
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116482597.001.png 116482597.002.png
Molecular Biology in Medicinal Chemistry
Edited by Th. Dingermann, D. Steinhilber and G. Folkers
116482597.003.png
Series Editors:
9
This book was carefully produced. Never-
theless, authors, editors and publisher
do not warrant the information contained
therein to be free of errors. Readers are
advised to keep in mind that statements,
data, illustrations, procedural details or
other items may inadvertently be
inaccurate.
Prof. Dr. Raimund Mannhold
Biomedical Research Center
Molecular Drug Research Group
Heinrich-Heine-Universit¨t
Universit¨tsstraße 1
40225 D¨sseldorf
Germany
raimund.mannhold@uni-duesseldorf.de
Library of Congress Card No. applied for
British Library Cataloguing-in-Publication
Data: A catalogue record for this book is
available from the British Library
Die Deutsche Bibliothek – CIP
Cataloguing-in-Publication-Data: A
catalogue record for this publication is
available from Die Deutsche Bibliothek
Prof. Dr. Hugo Kubinyi
BASF AG Ludwigshafen
c/o Donnersbergstraße 9
67256 Weisenheim am Sand
Germany
kubinyi@t-online.de
Prof. Dr. Gerd Folkers
Department of Applied Biosciences
ETH Z¨rich
Winterthurerstr. 190
8057 Z¨rich
Switzerland
folkers@pharma.anbi.ethz.ch
2004 WILEY-VCH Verlag GmbH & Co.
KGaA, Weinheim
All rights reserved (including those of
translation into other languages). No part of
this book may be reproduced in any form –
by photoprinting, microfilm, or any other
means – nor transmitted or translated into
a machine language without written
permission from the publishers. Registered
names, trademarks, etc. used in this book,
even when not specifically marked as such,
are not to be considered unprotected by law.
Volume Editors:
Prof. Dr. Theodor Dingermann
Institute of Pharmaceutical Biology
Johann Wolfgang Goethe-University
Marie-Curie-Str. 9
60439 Frankfurt
Germany
dingermann@em.uni-frankfurt.de
Printed in the Federal Republic of
Germany.
Printed on acid-free paper
Prof. Dr. Dieter Steinhilber
Institute of Pharmaceutical Chemistry
Johann Wolfgang Goethe-University
Marie-Curie-Str. 9
60439 Frankfurt
Germany
steinhilber@em.uni-frankfurt.de
Typesetting: Asco Typesetters, Hong Kong
Printing: betz-druck gmbh, Darmstadt
Bookbinding: Litges & Dopf Buchbinderei
GmbH, Heppenheim
ISBN 3-527-30431-2
Prof. Dr. Gerd Folkers
Department of Applied Biosciences
ETH Z¨rich
Winterthurerstr. 190
8057 Z¨rich
Switzerland
folkers@pharma.anbi.ethz.ch
(
v
Contents
Preface xv
Foreword xvii
Contributors xix
Part I Molecular Targets 1
1 Cellular Assays in Drug Discovery 3
Hugo Albrecht, Daniela Brodbeck-Hummel, Michael Hoever, Beatrice Nickel and
Urs Regenass
1.1 Introduction 3
1.1.1 Positioning Cellular Assays 3
1.1.2 Impact on Drug Discovery 4
1.1.3 Classification of Cellular Assays 5
1.1.4 Progress in Tools and Technologies for Cellular Compound Profiling 7
1.2 Membrane Proteins and Fast Cellular Responses 8
1.2.1 Receptors 8
1.2.1.1 FLIPR Technology for Detection of Intracellular Calcium Release 9
1.2.1.2 Competitive Immunoassay for Detection of Intracellular cAMP 9
1.2.1.3 Enzyme Fragment Complementation (EFC) Technology 12
1.2.2 Membrane Transport Proteins 12
1.2.2.1 Ion Channels 13
1.2.2.2 MDR Proteins 16
1.3 Gene and Protein Expression Profiling in High-throughput Formats 17
1.3.1 Reporter Gene Assays in Lead Finding 17
1.3.2 Reporter Gene Assays in Lead Optimization 21
1.4 Spatio-temporal Assays and Subpopulation Analysis 24
1.4.1 Phosphorylation Stage-specific Antibodies 25
1.4.2 Target-protein-specific Antibodies 26
1.4.3 Protein–GFP Fusions 27
1.4.4 Fluorescence Resonance Energy Transfer (FRET) 29
1.4.5 GPCR Activation using Bioluminescence Resonance Energy Transfer
(BRET) 31

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