Experimental Approaches to Rapid Identification, Profiling, and Characterization of Specific Biological Effects of DOS Compounds

Abstract

The spectrum of biological activity of any given diversity-oriented synthesis (DOS) compound is an unknown and a priori unforeseeable property; it has to be established through extensive experimental testing against a diverse panel of biological targets. This chapter focuses on the experimental approaches to rapid identification, profiling, and characterization of specific biological effects of DOS compounds. Testing sizable compound collections is performed in the confines of high-throughput screening (HTS). The main goal HTS is the identification of lead compounds with a desired specific set of properties. Diverse biological processes such as cell death, translational activity of genes, enzyme activity, and protein—protein interactions can be characterized in HTS assays reliably and quantitatively. These processes could be coupled with a variety of detection signals, resulting in a wide diversity of HTS assays. The major groups of HTS assays, together with their detection techniques and biological phenomena, are discussed in this chapter.