Target Identification and Validation in Drug Discovery

1. Front Matter

   Pages i-xiii

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2. Identification of Novel Targets Using High Throughput Screening Assays

   1. Front Matter

      Pages 1-1

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   2. Using Functional Genetics in Haploid Cells for Drug Target Identification

      • Jennifer C. Volz, Nicole Schuller, Ulrich Elling

      Pages 3-21

   3. Unbiased Forward Genetic Screening with Chemical Mutagenesis to Uncover Drug–Target Interactions

      • Moritz Horn, Franziska Metge, Martin S. Denzel

      Pages 23-31

   4. Integration of RNAi and Small Molecule Screens to Identify Targets for Drug Development

      • Konstantinos Drosopoulos, Spiros Linardopoulos

      Pages 33-42

   5. CellProfiler and KNIME: Open-Source Tools for High-Content Screening

      • Martin Stöter, Antje Janosch, Rico Barsacchi, Marc Bickle

      Pages 43-60

3. Drug Target Profiling and Validation

   1. Front Matter

      Pages 61-61

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   2. In Silico Target Druggability Assessment: From Structural to Systemic Approaches

      • Jean-Yves Trosset, Christian Cavé

      Pages 63-88

   3. In Silico Drug–Target Profiling

      • Jean-Yves Trosset, Christian Cavé

      Pages 89-103

   4. Locus-Specific Knock-In of a Degradable Tag for Target Validation Studies

      • Matthias Brand, Georg E. Winter

      Pages 105-119

   5. Expression of Human VH Single Domains as Fc Fusions in Mammalian Cells

      • Mahmoud Abdelatti, Peter Schofield, Daniel Christ

      Pages 121-136

4. Three Dimensional Cell Culture Techniques Mimicking the Tumor Microenvironment In Vitro

   1. Front Matter

      Pages 137-137

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   2. The Neurosphere Assay (NSA) Applied to Neural Stem Cells (NSCs) and Cancer Stem Cells (CSCs)

      • Rossella Galli

      Pages 139-149

   3. 3D-3 Tumor Models in Drug Discovery for Analysis of Immune Cell Infiltration

      • Annika Osswald, Viola Hedrich, Wolfgang Sommergruber

      Pages 151-162

   4. Establishment and Analysis of a 3D Co-Culture Spheroid Model of Pancreatic Adenocarcinoma for Application in Drug Discovery

      • Julia C. Meier-Hubberten, Michael P. Sanderson

      Pages 163-179

5. Animal Models for the Study of Gene Function In Vivo

   1. Front Matter

      Pages 181-181

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   2. In Vivo Pharmacology Models for Cancer Target Research

      • Dawei Chen, Xiaoyu An, Xuesong Ouyang, Jie Cai, Demin Zhou, Qi-Xiang Li

      Pages 183-211

   3. Use of CRISPR/Cas9 for the Modification of the Mouse Genome

      • Alexander Klimke, Steffen Güttler, Petric Kuballa, Simone Janzen, Sonja Ortmann, Adriano Flora

      Pages 213-230

   4. Assessment of Gene Function of Mouse Innate Lymphoid Cells for In Vivo Analysis Using Retroviral Transduction

      • Cyril Seillet, Gabrielle T. Belz

      Pages 231-240

   5. Creation of PDX-Bearing Humanized Mice to Study Immuno-oncology

      • Li-Chin Yao, Ken-Edwin Aryee, Mingshan Cheng, Pali Kaur, James G. Keck, Michael A. Brehm

      Pages 241-252

This second edition book explores breakthrough technologies in the field of drug target identification and validation. The volume emphasizes particularly revolutionary technologies, such as CRISPR-related screening, “big data,” and in silico approaches, as well as in vivo applications of CRISPR and best uses of animal models in drug development. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. 

Fully updated and authoritative, Target Identification and Validation in Drug Discovery: Methods and Protocols, Second Edition is an ideal guide for molecular and cellular biologists, pharmacologists, pathologists, bioinformaticians, clinical researchers, or investigators, as well as experts in other fieldsthat need a quick overview of these state-of-the-art technologies.

• Drug development
• CRISPR technologies
• Gene function
• Animal models
• Pharmacodynamics
• Biomarkers
• Pharmaceutical properties

• Pharmacology and Translational Research, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria

  Jürgen Moll

• Department of Cancer Cell Signaling, Boehringer Ingelheim RCV GmBH & Co KG, Vienna, Austria

  Sebastian Carotta

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