Design and pharmacology of peptide mimetics.

Publisher Summary This chapter analyzes the revolutionary changes that are at the forefront of the new pharmaceutical era, and also attempts to extrapolate the likely outcomes in the not-too-distant future. Although new conceptual and technological advances in the area of biomolecule mimetics includes all conceivable types of biomolecules, the most prolific effects both in the short and long terms is expected in the area of peptide mimetics because of the widespread distribution of peptides at the active sites of proteins including receptors, enzymes, antibodies, and so on. In fact the main thrust of the new technologies revolves around the ability to invoke a strategy of epitope identification, modeling, and mimicry, which is able to focus on a single biomolecule of interest, thus changing the scenario from random screening to targeted screening. A fairly ordered process is beginning to emerge for obtaining a peptide mimetic from a protein or biological peptide, which is outlined in the chapter. The interpretation of pharmacological data for peptide mimetics, such as the peptides themselves, is complicated by a number of factors including multiple binding sites, receptor subtypes, and issues relating to receptor cooperativity. Small-molecule mimetics may invoke another layer of complexity because of interactions with restricted binding sites not available to peptides, as well as effects resulting from increased membrane solubility.