Biomedical Engineering Reference
In-Depth Information
10
-12
mol l
-1
for homogeneous assays [346].FCS can be used for both,studies on
molecular interactions in solution based systems,or in cells performing assay
times in the second range.The application of FCS in accelerated HTS processes
is currently demonstrated by the German start-up company Evotec.
5.3
Sample Supply in High-Throughput Screening
Regarding current capacities of primary screening assays realized in HTS
attempts,it has become evident that high sample numbers to feed the assays are
needed. Combinatorial chemistry and the exploitation of molecular diversity
derived from biodiversity currently offer the greatest promise of finding novel
lead structures for significant therapeutic areas [4, 347, 348]. Especially new
chemical entities (NCEs) are required in order to facilitate therapeutic innova-
tions. Today, in the pharmaceutical industry, chemical libraries consisting of
at least 100,000 single compounds and libraries generated by combinatorial
chemistry approaches are routinely submitted to HTS in order to identify new
lead structures valuable for drug development.At the moment, crude extracts
derived from natural sources, such as plants, fungi, bacteria, and marine or-
ganisms only play a minor role.
5.4
Automation to Accelerate Drug Discovery
The starting point for the development ofautomation concepts was in analytical
routine laboratories (e.g.analytical R&D and quality control) dealing with high
numbers of samples routinely to be analyzed by the application of standardized
operation procedures [349].In parallel,the first robot systems for research were
developed and these combine the key technology of liquid handling with the
movement of items through a defined space.
Up to the present,the tremendous development in soft- and hardware as well
as the needs of the customers in the rapid growing environment of drug dis-
covery have resulted in a kind of evolution in purchase,installation,and imple-
mentation of laboratory robotics. Reliability, reproducibility, flexibility, and
speed have been set to a high standard.Over the past 15 years,laboratory auto-
mation has grown from a novel technology to a powerful and easy-to-handle
tool and provides the basis for modern high-throughput drug screening ap-
proaches.
5.4.1
Economic Aspects
Optimization ofdrug discovery strategies is driven by the actual patent situation
(drug discovery and development 10 to 12 years;term of patent 20 years;expiry
of important patents in the next few years will cause drastic drops in turnover)
forcing the companies to shorten the time taken to bring a drug onto the market.
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