Abstract
The craving need for novel targets in drug discovery, as gateways toward the cure of poorly tractable and intractable diseases, is illustrated here. The first section covers biology-based target identification methods in drug discovery through the last few decades. It presents functional and positional cloning, massive DNA sequencing, systems biology, RNA interference, and CRISPR-Cas9 genome editing. The following section deals with chemistry in target identification. It underlines the role of chemical diversity in supporting the identification of therapeutic targets. It covers natural products as high content probes, target-based and phenotype-based screening, forward and reverse chemical genetics approaches using drug-like collections in target identification. The last section describes the discovery of monastrol and the identification of kinesin Eg5 as an example of successful chemistry-supported target identification.
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