Biomedical Engineering Reference
In-Depth Information
needed.The capacity can be up to 20 to 80 microplates while higher throughput
is achievable by making use of multiple units.
Although laboratory robotics is a well-established technology there exists a
need for further improvement and next-generation devices,the so-called ultra-
high-throughput screening (UHTS). The whole process of drug discovery is
being forced to test an even higher number of compunds and a faster turnover
of new assay systems.Starting in 1985,10,000 data points per target have been
produced per year. In 1990, the same amount was tested in a month, while in
1995 this was achieved in a period as short as a week.At present,there is a need
to generate 10,000 to 100,000 data points in one robotic system per day.To meet
these requirements, two approaches have actually been realized, the so-called
Allegro system from Zymark (with multiple plate movers),and systems which
revolve around microliter volume assays in 1,536-well microplates (Pharma-
copeia) [356].
5.4.5
Data-Handling
Data management in drug discovery is used to handle the acquisition,analysis,
report generation, and database functions of the drug discovery data. It is
responsible for compound,and microplate registration,compound tracking,as
well as inventory control [357].The data handling is also used for the coordina-
tion of sample generation (combinatorial or parallel synthesis [358], natural
product extraction etc.),sample preparation (mother-,and daughter plates etc.),
assay registration, microplate schedule, data recording from analytical instru-
ments (readers etc.),and data analysis.Finally,it is necessary to link biological
results with chemical structures in order to complete the structure/activity
relationship (SAR) feedback loop [359].
A key component to the success of any drug discovery program is the
integration of HTS and combinatorial chemistry with database management
and molecular diversity systems to yield an efficient and cost-effective method
oforganizing chemical information and biological data.The ongoing increase in
throughput has created a substantial data management bottleneck. Further-
more,there are no standards for vendors for control software or file formats.
This leaves a gap between the laboratory equipment and the database that can
only be filled through custom programming.In comparison to the whole high-
throughput screening process,the set-up and management of the data handling
is cost-,and personal intensive.
6
Discussions and Conclusions
6.1
Natural Products
Currently,natural products are passing through a phase of reduced interest in
drug discovery because of the enormous efforts which are necessary to isolate
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