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Combinatorial Library

Methods and Protocols. 'Methods in Molecular Biology'. Auflage 2002. Book. Sprache: Englisch.
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The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms-such as apoptos … weiterlesen
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Titel: Combinatorial Library

ISBN: 0896039803
EAN: 9780896039803
Methods and Protocols.
'Methods in Molecular Biology'.
Auflage 2002.
Book.
Sprache: Englisch.
Herausgegeben von Lisa B. English
Humana Press

22. August 2002 - gebunden - 400 Seiten

Beschreibung

The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms-such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules-has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.

Inhaltsverzeichnis

Part I. Library Synthesis and Quality Control

Using a Noncovalent Protection Strategy to Enhance Solid-Phase Synthesis
Fahad Al-Obeidi, John F. Okonya, Richard E. Austin, and Dan R. S. Bond

Quality Control of Solid-Phase Synthesis by Mass Spectrometry
Jean-Louis Aubagnac, Robert Combarieu, Christine Enjalbal, and Jean Martinez

Preparation of Encoded Combinatorial Libraries for Drug Discovery
Tao Guo and Doug W. Hobbs

Simple Tools for Manual Parallel Solid Phase Synthesis
Viktor Krchnák and Andrew Burritt

Cleavage of Compounds from Solid Phase by Gaseous Reagents
Viktor Krchnák

Synthesis of DNA-Binding Polyamides: Robust Solid-Phase Methods for Coupling Heterocyclic Aromatic Amino Acids
Peter O. Krutzik and A. Richard Chamberlin

The Preparation of Phenyl-stilbene Derivatives Using the Safety Catch Linker
Amy Lew and A. Richard Chamberlin

Host-Guest Chemistry: Combinatorial Receptors
Brian R. Linton

Automated Structure Verification of Small Molecules Libraries Using 1D and 2D NMR Techniques
Gérard Rossé, Peter Neidig, and Harald Schröder

Rapid Liquid-Phase Combinatorial Synthesis of Heterocyclic Libraries
Chung-Ming Sun

Soluble Polymer-Supported Methods for Combinatorial and Organic Synthesis
Paul Wentworth, Jr. and Carsten Spanka

Analytical Methods for Optimization and Quality Control of Combinatorial Synthesis
Bing Yan, Liling Fang, Mark M. Irving, Jiang Zhao, Diana Liu, Gianine M. Figliozzi, Frank Woolard, and Clinton A. Krueger

Part II. Library Purification and Screening

Resolving Racemic Mixtures Using Parallel Combinatorial Libraries
Tingyu Li, Yan Wang, and Louis H. Bluhm

Ligand Libraries for the Extraction of Metal Ions: Dynamic Combinatorial and High-Throughput Screening Methods
Seema Choudhary and Janet R.Morrow

Automated Liquid-Liquid Extraction and Ion-Exchange Solid-Phase Extraction for Initial Purification
Sean X. Peng and Charles Henson

On-Bead and Solution Screening Approaches for Genomically Derived Targets: Discovery of Surrogate Ligands and Substrates Using Combinatorial Chemistry Libraries
David S. Thorpe, Gérard Rossé, Helen Yeoman, Sydney Wilson, Patti Willson, Greg Harlow, Anna Robinson, and Kenneth F. Wertman

Part III. Computational Library Design

Design of Virtual Combinatorial Libraries
Alex M. Aronov

Approaches to Library Design for Combinatorial Chemistry
Stefan Güssregen, Bernd Wendt, and Mark Warne

Reagent-Based and Product-Based Computational Strategies in Library Design
Eric A. Jamois

Designing Combinatorial Libraries for Efficient Screening
John I. Manchester and David S. Hartsough

Application of Neural Networks to Large Dataset QSAR, Virtual Screening, and Library Design
David A. Winkler and Frank R. Burden

Index

Pressestimmen

"...an excellent work that covers many important aspects, gives easy access to literature for further study, and contains much practical advice. As it describes many different tools and techniques it is especially suitable for beginners in combinatorial chemistry, and deserves to be added to the list of well presented works in this field." - Angewandte Chemie
"The book provides a wealth of excellent reference material and it is a worthwhile addition to the library of most medicinal chemists." -Journal of Medicinal Chemistry
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