Rankovic / Morphy Lead Generation Approaches in Drug Discovery

1. Auflage 2010
ISBN: 978-0-470-58416-3
Verlag: John Wiley & Sons
Format: PDF
Kopierschutz: Adobe DRM (»Systemvoraussetzungen)

E-Book, Englisch, 308 Seiten, E-Book

An integrated overview of modern approaches to leaddiscovery
Lead generation is increasingly seen as a distinct andsuccess-determining phase of the drug discovery process. Overrecent years, there have been major advances in the understandingof what constitutes a good lead compound and how to improve thechances of finding such a compound. Written by leading scientistsand established opinion leaders from industry and academia, thisbook provides an authoritative overview of the field, as well asthe theory, practice, and scope, of the principal LeadGeneration Approaches in Drug Discovery, including:
* The evolution of the lead discovery process, key concepts,current challenges, and future directions
* Strategies and technologies driving the high-throughputscreening (HTS) approach to lead discovery, including the shiftingparadigms in the design of compound collections and best practicein the hit confirmation process
* Knowledge-based in silico or "virtual" screening
* Theory and practice of the fragment-based approach to leaddiscovery
* The opportunities and challenges presented by multi-target drugdiscovery (MTDD)
* De novo design of lead compounds and new approaches toestimating the synthetic accessibility of de novo-designedmolecules
* The impact of natural products on drug discovery, and potentialof natural product-like compounds for exploring regions ofbiologically relevant chemical space
* Using early screening of hits and leads for metabolic,pharmacokinetic, and toxicological liabilities to reduce attritionduring the later phases of drug discovery
* The utility of parallel synthesis and purification in leaddiscovery
With each topic supported by numerous case studies, this isindispensable reading for researchers in industry and academia whowish to keep up to date with the latest strategies and approachesin drug discovery.

Autoren/Hrsg.

Rankovic, Zoran

Morphy, Richard

Inhaltsverzeichnis

PREFACE.
CONTRIBUTORS.
1 Lead Discovery: The Process (William F. Michne).
2 High Throughput Screening Approach to Lead Discovery (ZoranRankovic, Craig Jamieson, and Richard Morphy).
3 In Silico Screening (Dagmar Stumpfe, Hanna Geppert, andJürgen Bajorath).
4 Fragment-Based Lead Discovery (Jeffrey S. Albert).
5 Design of Multitarget Ligands (Richard Morphy and ZoranRankovic).
6 De novo Drug Design (Gisbert Schneider, MarkusHartenfeller, and Ewgenij Proschak).
7 Role of Natural Products in Drug Discovery (Hugo Lachance,Stefan Wetzel, and Herbert Waldmann).
8 Early Screening for ADMET Properties (Dennis A.Smith).
9 Role of Chemistry in Lead Discovery (Roland E. Dolle andKarin Worm).
INDEX.

Über Autor(innen)

ZORAN RANKOVIC is a Senior Research Fellow andAssociate Director in Medicinal Chemistry at Schering-PloughResearch Institute, UK. He received his PhD in organic chemistryfrom the University of Leeds (UK) before starting his medicinalchemistry career in 1995 at Organon, UK. Since then, working onprojects over a range of therapeutic areas, including psychosis,analgesia, and cardiovascular and bone diseases, he gainedextensive experience in all stages of the drug discovery process,including lead generation. From this work, Dr. Rankovic hasauthored or coauthored over fifty scientific publications, bookchapters, and patents, and has given invited lectures at numerousinternational conferences.
RICHARD MORPHY is a medicinal chemistry section head atSchering-Plough Research Institute (SPRI) at Newhouse, Scotland. Hehas twenty years' experience in the pharmaceutical industry,previously working for Celltech and Organon on a wide range ofoncology, inflammation, psychiatry, and analgesia projects. Inaddition to his extensive experience of the lead discovery process,he has a keen interest in the development of medicinal chemistry inemerging economies and is an opinion leader in the area ofmulti-target drug discovery.