Novel detection strategies for drug discovery

The Human Genome Project is expected to increase the number of potential drug targets from the current figure of 500 to ∼3000–4000. This increased number of targets, and increasing knowledge of signaling-pathway networks and their complexities, sets new demands for efficiency on HTS assay technologi...

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Bibliographic Details
Published in:Drug discovery today 2002-09, Vol.7 (18), p.S150-S156
Main Authors: Hemmilä, Ilkka A., Hurskainen, Pertti
Format: Article
Language:English
Subjects:
Animals
cAMP
DELFIA
FRET
Functional assays
GTP
Human Genome Project
Humans
Internalization
IP3
Ligands
Pharmacology - trends
Receptor trafficking
Receptors, Drug - drug effects
Receptors, Drug - genetics
Signal Transduction - genetics
β-Arrestin
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Summary:The Human Genome Project is expected to increase the number of potential drug targets from the current figure of 500 to ∼3000–4000. This increased number of targets, and increasing knowledge of signaling-pathway networks and their complexities, sets new demands for efficiency on HTS assay technologies. Assessment of the total efficacy of a given drug candidate requires not only the classical assays, but also a wide variety of assays related to signaling cascades and cellular functions. Discrete functional assays traditionally involved Ca2+ flux, kinases and cAMP, but today extend to the whole signaling network, from ligand binding to expression. This review discusses emerging novel non-radioisotopic assays, such as ligand-stimulated GTP-binding, the inositol triphosphate assay, cellular receptor trafficking, and protein–protein interactions.
ISSN:1359-6446
1878-5832
DOI:10.1016/S1359-6446(02)02390-5