A A Rationale for New Methods in Drug Discovery

The dramatic increase simultaneously, in the number of targets and the potential hit compounds is the reason for what has been called a change in paradigm in drug discovery [1]. To capitalize fully on the promise of both genomics and combinatorial chemistry, the drug discovery process must change in a fundamental way.

Rather than screening a limited number of chemical compounds against a particular target, combinatorial approaches often require screening thousands of compounds. Because of the preponderance of targets, screening must take place in days rather than months. Out of necessity, high-throughput screening (HTS) will be a key factor in realizing the potential of new drug discovery strategies by building a bridge between the increased number of targets and the vast number of compounds to be screened.

Not only does screening throughput need to be increased but also novel assay techniques and detection technologies have to be employed in order to provide more information about the suitability of specific compounds earlier in the screening process. This combination of quality and quantity must be achieved in order to take full advantage of the increased potential for target identification offered by genomics and proteomics and the potential for direct rapid access to novel chemical compounds offered by combinatorial chemistry and combinato-

B-12 years

Figure 1 A comparison of today's and tomorrow's drug discovery paradigm.

B-12 years

Figure 1 A comparison of today's and tomorrow's drug discovery paradigm.

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