Abstract
Combinatorial chemistry is a rapidly developing field. It is now considered as one of the most important recent advances in medicinal chemistry. In addition to drug lead identification, combinatorial chemistry can also be applied to the optimization of the initial lead. Most pharmaceutical companies have been focusing their efforts on small-molecule library development because drug leads discovered from these libraries are more likely to be able to cross cellular membranes. Therefore, for intracellular targets, small-molecule libraries are preferred. However, for extracellular targets, particularly those with larger natural ligands such as insulin, growth factors, and cytokines, peptide or oligomeric non-peptide libraries may sometimes be very useful, since it is unlikely that a small molecule (e.g., MW 300–600) can bind to these receptors with high affinity. Peptide libraries are also useful for the development of drug leads for enzymes that use peptides as a substrate, e.g., protease, and protein kinase. These peptide drug leads can then be converted to active peptidomimetics. The development of drugs for peptide hormone receptors, and vaccines for both humoral and cellular immunity certainly are two additional areas where peptide libraries will play an important role.
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Zhao, ZG., Lam, K.S. (1997). Synthetic peptide libraries. In: Moos, W.H., Pavia, M.R., Kay, B.K., Ellington, A.D. (eds) Annual Reports in Combinatorial Chemistry and Molecular Diversity. Annual Reports in Combinatorial Chemistry and Molecular Diversity, vol 1. Springer, Dordrecht. https://doi.org/10.1007/978-0-306-46904-6_14
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