Pseudo-Peptides In Drug Discovery

Peptides are among the most versatile bioactive molecules, yet the do not make good drugs, because they are quickly degraded or modified in the body.

To overcome this problem, stable and at the same time biologically active pseudo-peptides have been developed. These novel compounds open up new perspectives in drug design by providing an entire range of highly specific and non-toxic pharmaceuticals.

This is the first work devoted to the topic and draws together knowledge gained on different types of peptidomimetics and other pseudo-peptides with drug properties. As such, it includes peptoids, beta-peptides, polyamide DNA binders as well as peptide nucleic acids.

The expert authors and editor discuss chemical properties and stability, biological activity and reactivity, as well as practical aspects of synthesis, making this a prime resource for drug developers and bioorganic chemists working with these compounds.

Peter E. Nielsen has been affiliated with the University of Copenhagen (Denmark) since 1980, and he became full professor at the Department of Medical Biochemistry and Genetics in 1995. He is one of the inventors of peptide nucleic acid (1991), and has further studied and developed this DNA mimic during the last 12 years. In 1998 he co-founded Pantheco A/S (now Santaris A/S), a small biotech company based in Denmark. Peter Nielsen is the co-author of more than 275 scientific papers and 30 patents and patent applications. He received his Ph.B. in 1980 from the University of Copenhagen and an honoroary doctoral degree in 1990. He has also received several scientific awards and is a member of EMBO.

Preface.

List of Contributors.

1. Versatile Oligo(N-Substituted) Glycines: The Many Roles of Peptoids in Drug Discovery (J. Patch, et al.).

2. ß-Peptides, y-Peptides and Isosteric Backbones: New Scaffolds with Controlled Shapes for Mimicking Protein Secondary Structure Elements (G. Guichard).

3. Regulation of Gene Expression with Pyrrole-Imidazole Polyamides (P. Dervan, et al.).

4. Peptide Nucleic Acid (PNA): A Pseudo-peptide with DNA-like Properties (P. Nielsen, et al.).

5. a-Helical Peptide Nucleic Acids (aPNAs) (P. Garner, et al.).

6. DNA and RNA-cleaving Pseudo-peptides (A. Scarso & P. Scarso).

Subject Index.