Peptidomimetics – A Versatile Route to Biologically Active Compounds

Abstract

Abstract Proteins are vital for basically every known organism. Therefore the investigation of their structure, the development of a deeper understanding of protein–protein interactions and the design of novel peptides, which selectively interact with proteins are fields of active research. Small peptides consisting of the 20 natural amino acids typically show high conformational flexibility and a low in‐vivo stability which hampers their application as tools in medicinal diagnostics or molecular biology. One very versatile strategy to overcome such drawbacks is the use of peptidomimetics. These are small molecules which mimic natural peptides or proteins and thus produce the same biological effects as their natural role models. As the field of peptidomimetics is developing fast this review can only provide selected approaches together with examples and is not intended to be comprehensive. We focus on the discussion of amino acid modifications, backbone modifications, global restrictions by cyclisation and on synthetic backbone scaffolds. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)