John Dickenson, Fiona Freeman, Chris Lloyd Mills, Christian Thode, Shiva Sivasubramaniam

Molecular Pharmacology (eBook, ePUB)

From DNA to Drug Discovery

• Format: ePub

Produktbeschreibung

This textbook provides a fresh, comprehensive and accessible introduction to the rapidly expanding field of molecular pharmacology. Adopting a drug target-based, rather than the traditional organ/system based, approach this innovative guide reflects the current advances and research trend towards molecular based drug design, derived from a detailed understanding of chemical responses in the body. Drugs are then tailored to fit a treatment profile, rather than the traditional method of 'trial and error' drug discovery which focuses on testing chemicals on animals or cell cultures and matching their effects to treatments. Providing an invaluable resource for advanced under-graduate and MSc/PhD students, new researchers to the field and practitioners for continuing professional development, Molecular Pharmacology explores; recent advances and developments in the four major human drug target families (G-protein coupled receptors, ion channels, nuclear receptors and transporters), cloning of drug targets, transgenic animal technology, gene therapy, pharmacogenomics and looks at the role of calcium in the cell. * Current - focuses on cutting edge techniques and approaches, including new methods to quantify biological activities in different systems and ways to interpret and understand pharmacological data. * Cutting Edge - highlights advances in pharmacogenomics and explores how an individual's genetic makeup influences their response to therapeutic drugs and the potential for harmful side effects. * Applied - includes numerous, real-world examples and a detailed case-study based chapter which looks at current and possible future treatment strategies for cystic fibrosis. This case study considers the relative merits of both drug therapy for specific classes of mutation and gene therapy to correct the underlying defect. * Accessible - contains a comprehensive glossary, suggestions for further reading at the end of each chapter and an associated website that provides a complete set of figures from within the book.

---

Dieser Download kann aus rechtlichen Gründen nur mit Rechnungsadresse in A, B, BG, CY, CZ, D, DK, EW, E, FIN, F, GR, HR, H, IRL, I, LT, L, LR, M, NL, PL, P, R, S, SLO, SK ausgeliefert werden.

Produktdetails

• Verlag: John Wiley & Sons
• Seitenzahl: 424
• Erscheinungstermin: 30. November 2012
• Englisch
• ISBN-13: 9781118451953
• Artikelnr.: 37343900

Autorenporträt

John Dickenson, Fiona Freeman, Chris Lloyd Mills, Shiva Sivasubramaniam and Christian Thode, all at Nottingham Trent University.

Inhaltsangabe

Preface ix Abbreviations x 1 Introduction to Drug Targets and Molecular
Pharmacology 1 1.1 Introduction to molecular pharmacology 1 1.2 Scope of
this textbook 2 1.3 The nature of drug targets 3 1.4 Future drug targets 7
1.5 Molecular pharmacology and drug discovery 11 References 12 2 Molecular
Cloning of Drug Targets 13 2.1 Introduction to molecular cloning - from DNA
to drug discovery 13 2.2 'Traditional' pharmacology 14 2.3 The relevance of
recombinant DNA technology to pharmacology/drug discovery 14 2.4 The
'cloning' of drug targets 15 2.5 What information can DNA cloning provide?
20 2.6 Comparing the pharmacologic profile of the 'cloned' and the 'native'
drug target 23 2.7 Reverse pharmacology illustrated on orphan GPCRs 24 2.8
Summary 27 References 27 3 G Protein-coupled Receptors 31 3.1 Introduction
to G protein-coupled receptors 31 3.2 Heterotrimeric G-proteins 36 3.3
Signal transduction pathways 40 3.4 Desensitisation and down-regulation of
GPCR signalling 44 3.5 Constitutive GPCR activity 45 3.6 Promiscuous
G-protein coupling 47 3.7 Agonist-directed signalling 48 3.8 Allosteric
modulators of GPCR function 49 3.9 Pharmacological chaperones for GPCRs 50
3.10 GPCR dimerisation 51 3.11 GPCR splice variants 63 3.12 Summary 67
References 67 Useful Web sites 70 4 Ion Channels 71 4.1 Introduction 71 4.2
Voltage-gated ion channels 73 4.3 Other types of voltage-gated ion channels
89 4.4 Ligand-gated ion channels 109 4.5 Summary 125 References 125 5
Transporter Proteins 129 5.1 Introduction 129 5.2 Classification 129 5.3
Structural analysis of transporters 132 5.4 Transporter families of
pharmacological interest 133 5.5 Transporters and cellular homeostasis 167
5.6 Summary 169 References 169 6 Cystic Fibrosis: Alternative Approaches to
the Treatment of a Genetic Disease 175 6.1 Introduction 175 6.2 Cystic
fibrosis transmembrane conductance regulator 179 6.3 Mutations in CFTR 183
6.4 Why is cystic fibrosis so common? 184 6.5 Animal models of Cystic
fibrosis 186 6.6 Pharmacotherapy 186 6.7 Gene therapy 191 6.8 Conclusion
195 References 196 7 Pharmacogenomics 201 7.1 Types of genetic variation in
the human genome 201 7.2 Thiopurine S-methyltransferase and K+ channel
polymorphisms 202 7.3 Polymorphisms affecting drug metabolism 204 7.4
Methods for detecting genetic polymorphisms 209 7.5 Genetic variation in
drug transporters 211 7.6 Genetic variation in G protein coupled receptors
215 7.7 Summary 225 References 225 Useful Web sites 226 8 Transcription
Factors and Gene Expression 227 8.1 Control of gene expression 227 8.2
Transcription factors 229 8.3 CREB 233 8.4 Nuclear receptors 238 8.5
Peroxisome proliferator-activated receptors 240 8.6 Growth factors 247 8.7
Alternative splicing 247 8.8 RNA editing 251 8.9 The importance of
non-coding RNAs in gene expression 257 8.10 Summary 270 References 271 9
Cellular Calcium 277 9.1 Introduction 277 9.2 Measurement of calcium 278
9.3 The exocrine pancreas 289 9.4 Calcium signalling in pancreatic acinar
cells 292 9.5 Nuclear calcium signalling 303 9.6 Conclusions 310 References
311 10 Genetic Engineering of Mice 315 10.1 Introduction to genetic
engineering 315 10.2 Genomics and the accumulation of sequence data 315
10.3 The mouse as a model organism 318 10.4 Techniques for genetic
engineering 319 10.5 Examples of genetically-engineered mice 332 10.6
Summary 334 References 334 11 Signalling Complexes: Protein-protein
Interactions and Lipid Rafts 339 11.1 Introduction to cell signalling
complexes 339 11.2 Introduction to GPCR interacting proteins 340 11.3
Methods used to identify GPCR interacting proteins 340 11.4 Functional
roles of GPCR interacting proteins 345 11.5 GPCR signalling complexes 348
11.6 GPCR and ion channel complexes 355 11.7 Ion channel signalling
complexes 356 11.8 Development of pharmaceuticals that target GPCR
interacting proteins 356 11.9 Development of pharmaceuticals that target
protein-protein interactions 356 11.10 Lipid rafts 357 11.11
Receptor-mediated endocytosis 361 11.12 Summary 364 References 364 12
Recombinant Proteins and Immunotherapeutics 367 12.1 Introduction to
immunotherapeutics 367 12.2 Historical background of immunotherapeutics 368
12.3 Basis of immunotherapeutics 368 12.4 Types of immunotherapeutics 369
12.5 Humanisation of antibody therapy 372 12.6 Immunotherapeutics in
clinical practice 376 12.7 Advantages and disadvantages of immunotherapy
378 12.8 The future 379 12.9 Summary 380 References 380 Glossary 381 Index
403

Rezensionen

"An informative, comprehensive text, it is highly recommended to postgraduates and researchers in both pharmacology and molecular biology." (Science Progress, 1 March 2014)

"Overall, it could be the basis of an excellent course for junior pharmacologists in basic science research who need a greater focus on the mechanisms of drug action rather than an encyclopedic survey of clinical drug use." (Doody's, 26 July 2013)