Lead identification technologies

The so-called King-System is one of the technologies of choice for ambitious screening programs in the gas phase useful for fast lead identification. 

It was during the 1970 s and early 80 s that advances in technology transformed natural product discovery programmes. The advent of HPLC, and later coupling to UV diode-array detectors and then mass spectrometers, improved the efficiency of dereplication procedures. The ability to rapidly separate complex mixtures reduced the time from lead identification to natural product structure. The discovery of doramectin is a fine example of the use of such technology. 

In this chapter, we will describe the history and process of lead discovery from initial target identification and disease validation through the lead identification process itself, culminating in lead optimization and pre-clin-ical candidate selection. The full range of technologies and approaches that have been brought to bear on this complex activity will also be highlighted. 

Table 1.3-3 summarizes the most prevalent key technologies available today for lead identification of small molecules and macromolecules. This landscape is ever-... 

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