The identification of drug targets in a given disease has been central to pharmaceutical research from the latter half of the 20th century right up to the modern genomics era. Human Drug Targets provides an essential guide to one of the most important aspects of drug discovery the identification of suitable protein and RNA targets prior to the creation of drug development candidates. The first part of the book consists of introductory chapters that provide the background to drug target discovery and highlight the way in which these targets have been organised into online databases. It also includes a user s guide to the list of entries that forms the bulk of the book. Since this is not designed to be a compendium of drugs, the emphasis will be on the known (or speculated) biological role of the targets and not on the issues associated with pharmaceutical development. The objective is to provide just enough information to be informative and prompt further searches, while keeping the amount of text for each of the many entries to a minimum. Human Drug Targets will prove invaluable to those drug discovery professionals, in both industry and academia, who need to make some sense of the bewildering array of online information sources on current and potential human drug targets. As well as creating order out of a complex target landscape, the book will act as an ideas generator for potentially novel targets that might form the basis of future discovery projects.

The identification of drug targets in a given disease has been central to pharmaceutical research from the latter half of the 20th century right up to the modern genomics era. Human Drug Targets provides an essential guide to one of the most important aspects of drug discovery - the identification of suitable protein and RNA targets prior to the creation of drug development candidates.The first part of the book consists of introductory chapters that provide the background to drug target discovery and highlight the way in which these targets have been organised into online databases. It also includes a user's guide to the list of entries that forms the bulk of the book.Since this is not designed to be a compendium of drugs, the emphasis will be on the known (or speculated) biological role of the targets and not on the issues associated with pharmaceutical development. The objective is to provide just enough information to be informative and prompt further searches, while keeping the amount of text for each of the many entries to a minimum.Human Drug Targets will prove invaluable to those drug discovery professionals, in both industry and academia, who need to make some sense of the bewildering array of online information sources on current and potential human drug targets. As well as creating order out of a complex target landscape, the book will act as an ideas generator for potentially novel targets that might form the basis of future discovery projects.

Preface viiChapter 1 Introduction 11.1 Magic bullets 11.2 Background to modern pharmacology 21.2.1 The receptor theory 31.2.2 Molecular pharmacology 41.2.3 Receptors, signals and enzymes 41.2.4 Recombinant DNA technology and target discovery 51.3 Drug and therapeutic targets in the biomedical literature 51.4 How many drug targets are there? 51.4.1 Systematic target discovery 61.5 Screening for active molecules 7References 9Chapter 2 Overview of the drug target compendium 112.1 Introductory comments 112.2 Selection of entries 122.2.1 Gene name and symbol 122.2.2 Drug/investigational compound name 122.2.3 Literature reference 132.2.4 Involvement in disease 142.3 Organization of entries 152.3.1 Cell surface and secreted proteins 162.3.2 Enzymes 162.3.3 Entries classified by subcellular location 172.3.4 Non?]coding RNAs 182.4 Summary of data entries 182.5 How to use this book 192.6 Final comments 21References 21Chapter 3 Cell surface and secreted proteins 233.1 G?]protein?]coupled receptors (GPCRs) 243.1.1 G?]protein?]coupled receptor (GPCR) ligands 393.2 Nuclear hormone receptors (NHRs) 433.3 Cytokines and receptors 453.4 Adhesion molecules 643.5 Host defence molecules 753.6 Transporters and channels 903.6.1 ATP?]binding cassette families and transporting ATPases 903.6.2 Solute carrier (SLC) families 963.6.3 Ligand?]gated ion channels 1123.6.4 Voltage?]gated ion channels 1163.6.5 Assorted transport and carrier proteins 128Chapter 4 Enzymes: Part 1 1354.1 Signalling enzymes 1364.1.1 Protein kinases 1364.1.2 Protein phosphatases 1604.1.3 Cyclic nucleotides and phosphodiesterases 1684.1.4 GTPase signalling proteins 1704.1.5 Other signalling enzymes 1764.2 Protein modification 1794.2.1 Peptidases 1794.2.1.1 Peptidase inhibitors 2024.2.2 Glycosylation 2084.2.3 Ubiquitylation and related modifications 2184.2.4 Chromatin modification 2304.2.5 Protein synthesis and folding 2364.2.6 Other protein modifications 241Chapter 5 Enzymes: Part 2 2475.1 Lipids and related 2485.2 Amino acids and related 2675.3 Nucleotides and related 2765.4 Carbohydrates and related 2825.5 Vitamins, cofactors and related 2935.6 DNA?]processing enzymes 2965.7 RNA?]processing enzymes 3045.8 Stress response and homeostasis 3165.9 Miscellaneous enzymes 330Chapter 6 Remaining annotated entries grouped by subcellular location 3356.1 Cell surface and secreted proteins 3356.2 Cytoskeleton 3566.3 Cytoplasm to nucleus 3646.4 Nucleus 3756.5 Internal membranes and organelles 4006.6 Cytoplasmic proteins 4176.7 Subcellular location not annotated 424Chapter 7 Non?-Coding RNAs 437