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The application of high-throughput screening to novel lead discovery

Chapter
Part of the Progress in Drug Research book series (PDR, volume 51)

Summary

The ability to discover new lead compounds for novel therapeutic targets is a pivotal step in drug discovery programmes. High-throughput screening (HTS) utilises a number of platforms for the rapid screening of novel targets to accelerate this process. Key issues in HTS include assay configuration and the ability of a high-throughput screen to predict drug-target interactions accurately. This review highlights a number of issues in the HTS process and describes three key target areas that are likely to be sources of novel, therapeutically important drugs. Particular emphasis is placed on the mechanistic basis of drug-target interactions that are of prime importance in the design of HTS approaches. Critical aspects of information management related to HTS are summarised.

Keywords

High-throughput screening automation informatics receptors G-proteins ion channels kinases drug discovery orphan receptors 

Glossary of abbreviations

HTS

high-throughput screening

SPA

scintillation proximity assay

HTRF

homogeneous timeresolved fluorescence

ELISA

enzyme-linked immunoabsorbtion assay

GFP

green fluorescent protein

RTK

receptor tyrosine kinases

GPCR

G-protein-coupled receptor

EGRF

epidermal growth factor receptor

FRET

fluorescence resonance energy transfer

CRE

cyclic-AMP response element

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Copyright information

© Springer Basel AG 1998

Authors and Affiliations

  1. 1.Cambridge Drug DiscoveryCambridgeUK

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