Free Download Molecular Biology in Medicinal Chemistry by Th. Dingermann Vol. 21

Methods and Principles in Medicinal Chemistry

Volume 21

Authors of: Molecular Biology in Medicinal Chemistry by Th. Dingermann Vol. 21

Th. Dingermann

R. Mannhold

H. Kubinyi

D. Steinhilber and

G. Folkers

Table of Contents in Molecular Biology in Medicinal Chemistry by Th. Dingermann Vol. 21

Preface

Foreword

Contributors

Part I Molecular Targets

1 Cellular Assays in Drug Discovery

Hugo Albrecht, Daniela Brodbeck-Hummel, Michael Hoever, Beatrice Nickel and Urs Regenass

1.1 Introduction

1.1.1 Positioning Cellular Assays

1.1.2 Impact on Drug Discovery

1.1.3 Classification of Cellular Assays

1.1.4 Progress in Tools and Technologies for Cellular Compound Profiling

1.2 Membrane Proteins and Fast Cellular Responses

1.2.1 Receptors

1.2.1.1 FLIPR Technology for Detection of Intracellular Calcium Release

1.2.1.2 Competitive Immunoassay for Detection of Intracellular cAMP

1.2.1.3 Enzyme Fragment Complementation (EFC) Technology

1.2.2 Membrane Transport Proteins

1.2.2.1 Ion Channels

1.2.2.2 MDR Proteins

1.3 Gene and Protein Expression Profiling in High-throughput Formats

1.3.1 Reporter Gene Assays in Lead Finding

1.3.2 Reporter Gene Assays in Lead Optimization

1.4 Spatio-temporal Assays and Subpopulation Analysis

1.4.1 Phosphorylation Stage-specific Antibodies

1.4.2 Target-protein-specific Antibodies

1.4.3 Protein–GFP Fusions

1.4.4 Fluorescence Resonance Energy Transfer (FRET)

1.4.5 GPCR Activation using Bioluminescence Resonance Energy Transfer (BRET)

1.4.6 Protein Fragment Complementation Assays (PCA)

1.5 Phenotypic Assays

1.5.1 Proliferation/Respiration/Toxicity

1.5.2 Apoptosis

1.5.3 Differentiation

1.5.4 Monitoring Cell Metabolism

1.5.5 Other Phenotypic Assays

Acknowledgments

References

2 Gene Knockout Models

Peter Ruth and Matthias Sausbier

2.1 Introduction

2.2 Gene Knockout Mice

2.2.1 ES Cells

2.2.2 Targeting Vector

2.2.3 Selection of Recombinant ES Cells

2.2.4 Injection of Recombinant ES Cells into Blastocysts and Blastocyst Transfer to Pseudopregnant Recipients

2.2.5 Chimeras and F1 and F2 Offspring

2.3 Tissue-Specific Gene Expression

2.3.1 Ligand-Activated CRE Recombinases

2.3.2 The Tetracycline/Doxycycline-Inducible Expression System

2.4 Transgenic Mice

2.5 Targeted Gene Disruption in Drosophila

2.6 Targeted Gene Knockdown in Zebrafish

2.7 Targeted Caenorhabditis Elegans Deletion Strains

References

3 Reporter Gene Assay Systems for the Investigation of G-protein-coupled Receptors

Michaela C. Dinger and Annette G. Beck-Sickinger

3.1 Receptors and Cellular Communication

3.1.1 Ion Channel-linked Receptors

3.1.2 Enzyme-linked Cell-surface Receptors

3.1.3 GPCRs

3.2 Affinity and Activity of GPCR Ligands

3.3 The Role of Transcription Factors in Gene Expression

3.3.1 CREB

3.3.2 SRF

3.3.3 STAT Proteins

3.3.4 c-Jun

3.3.5 NF-AT

3.4 Reporter Genes

3.4.1 CAT

3.4.2 b-Gal

3.4.3 b-Glucuronidase

3.4.4 AP

3.4.5 SEAP

3.4.6 b-Lactamase

3.4.7 Luciferase

3.4.8 GFP

3.5 Reporter Gene Assay Systems for the Investigation of GPCRs

3.5.1 Application of Luciferase as a Reporter Gene

3.5.2 Application of other Reporter Genes for the Investigation of GPCRs

References

4 From the Human Genome to New Drugs: The Potential of Orphan G-protein￾coupled Receptors

Remko A. Bakker and Rob Leurs

4.1 Introduction

4.2 GPCRs and the Human Genome

4.2.1 GPCR Architecture, Signaling and Drug Action

4.2.2 Identification of GPCRs

4.2.3 GPCRs in the Postgenomic Era: Orphan Receptors

4.3 Ligand Hunting

4.3.1 Reverse Pharmacology Approaches to oGPCRs

4.3.2 In Silico Approaches

4.3.3 Tissue Expression

4.3.4 Expression of an oGPCR of Interest

4.3.5 Screening Approaches

4.4 Screening for oGPCR Ligands using Functional Assays

4.4.1 GTPgS-binding Assays

4.4.2 Measurements of cAMP

4.4.3 Ca2þ Measurements

4.4.4 The Cytosensor Microphysiometer

4.4.5 Reporter Gene Assays

4.4.6 GPCR–G-protein Coupling

4.4.7 Ligand-independent GPCR Activity

4.4.8 Novel Screening Strategies

4.5 Future Prospects

References

Part II Synthesis

5 Stereoselective Synthesis with the Help of Recombinant Enzymes

Nagaraj N. Rao and Andreas Liese

6 Nucleic Acid Drugs

Joachim W. Engels and Jo¨rg Parsch

Part III Analysis

7 Recent Trends in Enantioseparation of Chiral Drugs

Bezhan Chankvetadze

8 Affinity Chromatography

Gerhard K. E. Scriba

9 Nuclear Magnetic Resonance-based Drug Discovery

Ulrich L. Gu¨nther, Christina Fischer and Heinz Ru¨terjans

10 13C- and 15N-Isotopic Labeling of Proteins

Christian Klammt, Frank Bernhard and Heinz Ru¨terjans

11 Application of Antibody Fragments as Crystallization Enhancers

Carola Hunte and Cornelia Mu¨nke

Acknowledgments

References

Part IV Kinetics, Metabolism and Toxicology

12 Pharmacogenetics: The Effect of Inherited Genetic Variation on Drug

Disposition and Drug Response

Kurt Kesseler

13 Pharmacogenomics of Bioavailability and Elimination

Ingolf Cascorbi and Heyo K. Kroemer

14 Toxicogenomics: Integration of New Molecular Biological Tools in Toxicology

Wilbert H. M. Heijne, Ben van Ommen and Rob H. Stierum

References

Index  

File Size: 5.08 MB. Pages: 429. Please read Disclaimer.

Free download Molecular Biology in Medicinal Chemistry by Th. Dingermann Vol. 21

Download Link 1

You may also like to download “The Chemistry of Medical and Dental Materials by John W. Nicholson”.

Free download hundreds of chemistry books in pdf from HERE.

Please Subscribe to our Email list and get notified of our latest uploads (Books, documents) and new updates. Email Subscription Box is provided on the sidebar (for PC) and on the bottom of this post (for Android Devices).

Kindly Like, Follow and Share our social media pages so that maximum people can benefit from this public service!

Facebook   Instagram    LinkedIn    Twitter    Pinterest

P.S: If the download link(s) is/are not working, kindly drop a comment below, so we’ll update the download link for you.

Happy reading!