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Biomolecular screening
is an essential part in the early
phase of the drug discovery process.
Large numbers of organic molecules
are being tested in well defined biological
assay systems, with the purpose of
identifying the few molecules which
interact specifically with the protein target and could serve as starting points for
chemical lead optimization.
Molecules which show a significant
biological activity are further tested
and validated in a panel of functional
enzymatic or cellular assays.
The predominant assay readout systems are Ca flux
and membrane potential measurement assays for
receptor and ion channel targets and
kinetic assays, based on time-resolved
fluorescence, fluorescent energy transfer, luminescence or absorption
readings.
Protein-protein interactions are central
to many signaling pathways and are
studied with conventional ELISA technology
or with a novel detection system based
on electrochemiluminescence.
Analysis of intracellular protein aggregation events,
being the cause of many neurodegenerative
diseases, is now possible using high
content screening technology. |