Advances in Drug Research (eBook)

Front Cover 1
Advances in Drug Research 4
Copyright Page 5
Table of Contents 6
CONTRIBUTORS 8
PREFACE: "All mimsy were the borogoves" 9
Chapter 1. Atom Description in QSAR Models: Development and Use of an Atom Level Index 12
1 Introduction 13
2 An Atom Level Description of Structure 16
3 Formulation of an Atom-Centred Index 19
4 Information from Electrotopological State Values 26
5 QSAR Strategy 31
6 Applications to Drug QSAR Problems 34
7 Discussion 46
References 48
Chapter 2. Pharmacokinetics of Peptides and Proteins: Opportunities and Challenges 50
1 Introduction 52
2 Physicochemical Factors and Passive Distribution 65
3 Clearance 86
4 Transport of Peptides Across Mucosal Surfaces 103
5 Conclusions 109
References 112
Chapter 3. Towards Genomic Pharmacology: From Membranal to Nuclear Receptors 118
1 Introduction 119
2 Regulation of Gene Expression 120
3 Nuclear Receptors 126
4 Induced Changes in Gene Expression 135
5 The Nucleus as a Target for Drug Action 144
6 Signal Pathways: From Membrane to Nuclear Receptors 147
7 Future Prospects 153
Acknowledgements 154
References 154
Chapter 4. Medicinal Chemistry of Steroids: Recent Developments 160
1 Introduction 160
2 Steroid Receptors 161
3 Steroid-Converting Enzymes: The Case of 3-Oxo-.5-Steroid Isomerase 173
4 Inhibitors of Steroid-Converting Enzymes 179
5 Oestrogen Receptor-Based Imaging Agents 192
6 Conclusions and Future Developments 194
References 195
SUBJECT INDEX 202
CUMULATIVE INDEX OF AUTHORS 212
CUMULATIVE INDEX OF TITLES 214