Applications of Combinatorial Technologies to Drug Discovery. 1. Background and Peptide Combinatorial Libraries

Recent trends in the search for novel pharmacological agents have focused on the preparation of "chemical libraries" as potential sources of new leads for drug discovery. Chemical libraries are intentionally created collections of differing molecules which can be prepared either synthetically or biosynthetically and screened for biological activity in a variety of different formats (e.g., libraries of soluble molecules; libraries of compounds tethered to resin beads, silica chips, or other solid supports; recombinant peptide libraries on bacteriophage and other biological display vectors; etc). Combinatorial chemistry is a type of synthetic strategy which leads to large chemical libraries. For the purposes of this discussion, combinatorial chemistry may be defined as the systematic and repetitive, covalent connection of a set of different "building blocks" of varying structures to each other to yield a large array of diverse molecular entities.