High Throughput Screening for Novel Anti-Inflammatories

Overview

Combinatorial chemistry in conjunction with High Throughput Screening (HTS) is revolutionizing the drug discovery process. Yet, we have much to learn about the integration of these powerful techniques with info rmation from genomics, proteomics, computation and pharmacokinetics be fore dramatic increases in the drug discovery/development processes ca n be achieved. The chapters in this book represent the state of the ar t regarding the integration of combinatorial chemistry and HTS in conn ection with ...

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Overview

Combinatorial chemistry in conjunction with High Throughput Screening (HTS) is revolutionizing the drug discovery process. Yet, we have much to learn about the integration of these powerful techniques with info rmation from genomics, proteomics, computation and pharmacokinetics be fore dramatic increases in the drug discovery/development processes ca n be achieved. The chapters in this book represent the state of the ar t regarding the integration of combinatorial chemistry and HTS in conn ection with anti-inflammatory targets. Obviously, there is much work t o be done beyond what is described in this text, nevertheless, it shou ld set the stage for creative thinking among scientists of many discip lines for the accomplishment of our ultimate goals in treating inflamm atory diseases.

The book contains predominantly black-and-white illustrations, with some color illustrations.

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Editorial Reviews

Eugene A. Davidson
The latest technology involved in drug development involves combinatorial synthetic methods as a platform and high throughput screening for analysis. The ability to generate very large numbers of closely related compounds by organic or biosynthetic means has necessitated the development of rapid evaluation techniques designed to identify lead compounds for further development. This volume, a compilation of targets, is a presentation of current thinking in several areas. As such it is a useful albeit limited introduction to this research area. The purpose does not match what the title implies. Instead of screening methods, the editor presents information on compounds; the objectives therefore are not met. This volume can be recommended for those wishing an overview of limited scope in areas discussed. This will appeal mainly to investigators wishing an update on approaches to certain types of drugs. In the first chapter contributors review some combinatorial chemistry, largely based on solid supports, an approach pioneered by Mario Geysen. The subsequent chapter contributors discuss protease inhibitors, cell adhesion antagonists, and inhibitors of selected signal transduction pathways such as MAP kinase. The contributions focus on compounds rather than screening methods and hence the title is somewhat misleading. In addition, essentially all of the material contributed is from the private sector, which results in limited coverage of the fields involved. For example, the chapter on selectins has little to say about the combinatorial work in carbohydrates currently ongoing in several laboratories. There is insufficient attention given to the strategies behind screening methodsand the design of these for a particular target.
Doody's Review Service
Reviewer: Eugene A Davidson, PhD (Georgetown University School of Medicine)
Description: The latest technology involved in drug development involves combinatorial synthetic methods as a platform and high throughput screening for analysis. The ability to generate very large numbers of closely related compounds by organic or biosynthetic means has necessitated the development of rapid evaluation techniques designed to identify lead compounds for further development. This volume, a compilation of targets, is a presentation of current thinking in several areas. As such it is a useful albeit limited introduction to this research area.
Purpose: The purpose does not match what the title implies. Instead of screening methods, the editor presents information on compounds; the objectives therefore are not met.
Audience: This volume can be recommended for those wishing an overview of limited scope in areas discussed. This will appeal mainly to investigators wishing an update on approaches to certain types of drugs.
Features: In the first chapter contributors review some combinatorial chemistry, largely based on solid supports, an approach pioneered by Mario Geysen. The subsequent chapter contributors discuss protease inhibitors, cell adhesion antagonists, and inhibitors of selected signal transduction pathways such as MAP kinase.
Assessment: The contributions focus on compounds rather than screening methods and hence the title is somewhat misleading. In addition, essentially all of the material contributed is from the private sector, which results in limited coverage of the fields involved. For example, the chapter on selectins has little to say about the combinatorial work in carbohydrates currently ongoing in several laboratories. There is insufficient attention given to the strategies behind screening methods and the design of these for a particular target.

3 Stars from Doody
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Product Details

  • ISBN-13: 9783034895781
  • Publisher: Birkhauser Basel
  • Publication date: 11/1/2012
  • Series: Progress in Inflammation Research Series
  • Edition description: Softcover reprint of the original 1st ed. 2000
  • Pages: 258
  • Product dimensions: 6.14 (w) x 9.21 (h) x 0.58 (d)

Table of Contents

Solid phase synthesis: Applications to combinatorial libraries.- Proteasome inhibitors.- Caspase-1 (ICE) and other caspases as drug discovery targets: Opportunities and progress.- Elastase inhibitors.- A high throughput assay for the TNF converting enzyme.- Tryptase inhibitors.- Selectin antagonists.- Cell adhesion integrins as pharmaceutical targets.- Inhibitors of the MAPK pathway.- Inhibition of NF-?B.- IL-1 antagonist discovery.- Phosphodiesterase inhibitors for respiratory diseases.

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