High Throughput Screening for Novel Anti-Inflammatories

by Michael Kahn (Editor)

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 information from genomics, proteomics, computation and pharmacokinetics before dramatic increases in the drug discovery/development processes can be achieved. The chapters in this book represent the state of the art regarding the integration of combinatorial chemistry and HTS in connection with anti-inflammatory targets. Obviously, there is much work to be done beyond what is described in this text, nevertheless, it should set the stage for creative thinking among scientists of many disciplines for the accomplishment of our ultimate goals in treating inflammatory diseases.

Product Details

ISBN-13:	9783034895781
Publisher:	Birkhäuser Basel
Publication date:	11/01/2012
Series:	Progress in Inflammation Research
Edition description:	Softcover reprint of the original 1st ed. 2000
Pages:	258
Product dimensions:	6.10(w) x 9.25(h) x 0.02(d)

About the Author

Kahn, Michael (Univ of Washington)

Table of Contents

Contents. List of Contributors. Intoduction. Sharon M. Dankwardt: Solid phase synthesis: applications to combinatorial libraries. Mohamed A. Iqbal and Mark A. Ator: Proteaspme inhibitors. Tariq Ghayur, Sheryl J. Hays and Robert V. Talanian: Caspase-1 (ICE) and other caspases as drug discovery targets: opportunities and progress. William A. Metz and Norton P. Peet: Elastase inhibitors. M. Anthony Leesnitzer, D. Mark Bickett, Marcia L. Moss and J. David Becherer: A high-throughput assay for the TNF conerting enzyme. Kenneth D. Rice and William R. Moore: Tryptase inhibitors. Falguni Dasgupta: Selectin antagonists. Kerry W. Fowler and David T. Crowe: Cell adhesion integrins as pharmaceutical targets. Brion W. Murray, Yoshitaka Satoh and Bernd Stein: Inhibitors of the MAPK pathway. Mark J. Suto and Anthony M. Manning: Inhibition of NF-kB. Terry L. Bowlin, Stephen D. Yanofsky and Herman Schreuder: IL-1 antagonist discovery. Mark A. Giembycz: Phosphodiesterase inhibitors for respiratory disease. Subject index

Editorial Reviews

3 Stars from Doody

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.

Eugene A. Davidson

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.

Doody's Review Service