Abstract
Traditional drug discovery methods were slow and labor-intensive and limited the number and chemical diversity of the compounds and targets that can be screened in a given assay. Even though many thousands of distinct chemical structures exist, it is not unusual for screening utilizing this approach to be terminated at the end of several years with no lead compounds identified, having examined only a small fraction of available compounds. This limitation of speed and scale often restricts both the quality and quantity of lead compounds available for further testing and development, thereby hindering drug discovery. In an improvement of this approach, several “hits” are produced as a result of high-throughput screening (HTS). Hit-to-lead stage has been added to the drug discovery. Multiple parameters are optimized in parallel to produce leads with a balanced profile of biological and physicochemical properties. New technologies are playing an increasing role in this process. It is desirable to have multiple series in hit optimization so that more than one series is available for lead optimization (Jain 2009). Important biotechnologies that have been used for improving drug discovery are listed in Table 14.1. Most of the new drug development involves biotherapeutics.
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Jain, K.K. (2014). Biotechnology in Drug Discovery and Development for Cancer. In: Applications of Biotechnology in Oncology. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4614-9245-0_14
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