TURN AND HELIX MIMETICS FOR PEPTIDE DESIGN. Anke Mueller-Fahrnow & Ursula Egner, Research Laboratories of Schering AG, D-13342 Berlin, F.R.G.

Peptides play an important role in the regulation of a wide variety of biological functions, acting as hormones, neurotransmitters or inhibitors. The therapeutic use of peptides is often hampered by their lack of metabolic stability and their inadequate transport properties. To overcome these problems, the substitution of e.g. helices and turns with appropriate peptidomimetics has been tested.

To build up a database of peptidomimetics, we have performed a thorough search in the recent literature, classified the available beta-turn and helix mimetics according to different criteria and analyzed the results with respect to activity and structure elucidation via X-ray crystallography, NMR spectroscopy or modeling studies. We are currently in the process of incorporating these mimetics as easy to use building blocks in the library of our modeling software.

Although the interest in peptidomimetics is growing permanently and their usefulnes in modeling projects is not questioned, only a few beta- turn and helix mimetics have been published and even less characterized with respect to the three-dimensional structure, the potency and the binding mode. Moreover, the application of some of these compounds is restricted due to a time consuming or difficult

synthesis.

The opinions expressed above are solely those of the author and are not necessarily those of the Schering AG