Human Drug Targets

Preface vii
Chapter 1 Introduction 1
1.1 Magic bullets 1
1.2 Background to modern pharmacology 2
1.2.1 The receptor theory 3
1.2.2 Molecular pharmacology 4
1.2.3 Receptors, signals and enzymes 4
1.2.4 Recombinant DNA technology and target discovery 5
1.3 Drug and therapeutic targets in the biomedical literature 5
1.4 How many drug targets are there? 5
1.4.1 Systematic target discovery 6
1.5 Screening for active molecules 7
References 9
Chapter 2 Overview of the drug target compendium 11
2.1 Introductory comments 11
2.2 Selection of entries 12
2.2.1 Gene name and symbol 12
2.2.2 Drug/investigational compound name 12
2.2.3 Literature reference 13
2.2.4 Involvement in disease 14
2.3 Organization of entries 15
2.3.1 Cell surface and secreted proteins 16
2.3.2 Enzymes 16
2.3.3 Entries classified by subcellular location 17
2.3.4 Non?]coding RNAs 18
2.4 Summary of data entries 18
2.5 How to use this book 19
2.6 Final comments 21
References 21
Chapter 3 Cell surface and secreted proteins 23
3.1 G?]protein?]coupled receptors (GPCRs) 24
3.1.1 G?]protein?]coupled receptor (GPCR) ligands 39
3.2 Nuclear hormone receptors (NHRs) 43
3.3 Cytokines and receptors 45
3.4 Adhesion molecules 64
3.5 Host defence molecules 75
3.6 Transporters and channels 90
3.6.1 ATP?]binding cassette families and transporting ATPases 90
3.6.2 Solute carrier (SLC) families 96
3.6.3 Ligand?]gated ion channels 112
3.6.4 Voltage?]gated ion channels 116
3.6.5 Assorted transport and carrier proteins 128
Chapter 4 Enzymes: Part 1 135
4.1 Signalling enzymes 136
4.1.1 Protein kinases 136
4.1.2 Protein phosphatases 160
4.1.3 Cyclic nucleotides and phosphodiesterases 168
4.1.4 GTPase signalling proteins 170
4.1.5 Other signalling enzymes 176
4.2 Protein modification 179
4.2.1 Peptidases 179
4.2.1.1 Peptidase inhibitors 202
4.2.2 Glycosylation 208
4.2.3 Ubiquitylation and related modifications 218
4.2.4 Chromatin modification 230
4.2.5 Protein synthesis and folding 236
4.2.6 Other protein modifications 241
Chapter 5 Enzymes: Part 2 247
5.1 Lipids and related 248
5.2 Amino acids and related 267
5.3 Nucleotides and related 276
5.4 Carbohydrates and related 282
5.5 Vitamins, cofactors and related 293
5.6 DNA?]processing enzymes 296
5.7 RNA?]processing enzymes 304
5.8 Stress response and homeostasis 316
5.9 Miscellaneous enzymes 330
Chapter 6 Remaining annotated entries grouped by subcellular location 335
6.1 Cell surface and secreted proteins 335
6.2 Cytoskeleton 356
6.3 Cytoplasm to nucleus 364
6.4 Nucleus 375
6.5 Internal membranes and organelles 400
6.6 Cytoplasmic proteins 417
6.7 Subcellular location not annotated 424
Chapter 7 Non?-Coding RNAs 437