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.Peptide gehören zu den vielseitigsten bioaktiven Molekülen überhaupt. Trotzdem ist ihre Eignung als pharmazeutische Wirkstoffe beschränkt, da sie im Körper rasch abgebaut oder verändert werden.
Um dieses Problem zu lösen sind stabile und gleichzeitig biologisch aktive Pseudopeptide entwickelt worden.
Diese Verbindungen erschließen neue Perspektiven in der Medikamentenentwicklung und stellen eine ganze Palette neuartiger hochspezifischer und nicht-toxischer Pharmazeutika zur Verfügung.
Erstmalig ist hier das gesamte Wissen zusammengefasst, das über verschiedene Arten von Peptidomimetika und andere Pseudopeptide mit Einsatzmöglichkeiten in der Pharmaforschung gewonnen wurde.
Peptoide, Beta - Peptide, DNA-bindende Polyamide sowie Peptid-Nucleinsäuren werden hier behandelt.
Ausgewiesene Experten diskutieren chemische Eigenschaften und Stabilität, biologische Aktivität und Reaktivität, sowie praktische Aspekte der Synthese und machen dieses Werk damit zur essentiellen Informationsquelle für alle Medikamentenentwickler und bioorganische Chemiker, die mit diesen Verbindungen arbeiten. Versatile oligo-glycines: The many roles of peptoids in drug discovery
Beta-peptides, gamma-peptides and isosteric backbones: New scaffolds with controlled shapes
Regulation of gene expression with pyrrole-imidazole polyamides
Peptide nucleic acid: A pseudo-peptide with DNA-like properties
Alpha-helical peptide nucleic acids
DNA-cleaving pseudo-peptides
"... thoughtfully compiled and well-presented. Researchers working in these specific areas will want to own a copy of this book." (Journal of the American Chemical Society, February 23, 2005)

"... the editor of this book has brought together a number of excellent reviews for obtaining up-to-date information in the areas of research covered, and I highly recommend it." (Victor J. Hruby, Department of Chemistry, University of Arizona, Journal of Medicinal Chemistry, 2005, Vol. 48, No. 8)

"In view of the thoroughly up-to-date coverage of the topics in this book, it can be highly recommended for drug developers and bioorganic chemists working with pseudopeptides, and for all researchers who are interested in the field of nucleic acid chemistry." (Angewandte Chemie, Volume 43, Oct. 2004) "Das Buch stellt die wichtigsten Eigenschaften und die Vielseitigkeit der Pseudopeptide heraus, mit dem Ziel, neue Entwicklungen in der Wirkstoff-Forschung einzuleiten. Angesichts der aktuellen und detaillierten Darstellung der Themen kann die Lektüre ohne Einschränkung jedermann empfohlen werden, der in der Wirkstoff-Forschung tätig ist, sich mit Pseudopeptiden beschäftigt oder sich für die DNA-Forschung interessiert."

Kiyohiko Kawai, Institute of Scientific and Industrial Research, Universität Osaka, Angewandte Chemie, 2. Novemberheft 2004-116/42 und Angewandte Chemie International Edition, 2nd November Issue 2004-43/42 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. 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.
Thus, drug discovery has turned to the novel field of peptidomimetics, i. e. to design non-peptide compounds mimicking the pharmacophore and thus the activity of the original peptide. These novel compounds open up new perspectives in drug design by providing an entire range of highly specific pharmaceuticals that have a high bioavailability.
In particular, the following classes of pseudo-peptides are introduced and examined with regard to their chemical properties, pharmacological activity, as well as practical aspects of synthesis:

* Oligo-glycines
* Beta-peptides
* Gamma-peptides
* Pyrrole-imidazole polyamides
* DNA-like peptide nucleic acids
* Alpha-helical peptide nucleic acids
* DNA-cleaving pseudo-peptides

The first work drawing together knowledge gained on different types of pseudo-peptides with drug properties, this book is an essential resource for drug developers and bioorganic chemists working with those compounds.