Solid-phase synthetic route to multiple derivatives of a fundamental peptide unit.
Amino acids are Nature's combinatorial building blocks. When substituted on both the amino and carboxyl sides they become the basic scaffold present in all peptides and proteins. We report a solid-phase synthetic route to large combinatorial variations of this fundamental scaffold, extending the variety of substituted biomimetic molecules available to successfully implement the Distributed Drug Discovery (D3) project. In a single solid-phase sequence, compatible with basic amine substituents, three-point variation is performed at the amino acid a-carbon and the amino and carboxyl functionalities.
Scott
William L
WL
Department of Chemistry and Chemical Biology, Indiana University-Purdue University, Indianapolis, 402 N. Blackford Street, Indianapolis, IN 46202, USA. wscott@iupui.edu
Zhou
Ziniu
Z
Zajdel
Paweł
P
Pawłowski
Maciej
M
O'Donnell
Martin J
MJ
D020650:Combinatorial Chemistry Techniques; D055808:Drug Discovery; D018716:Molecular Mimicry; D019151:Peptide Library; D010455:Peptides / Q000138:chemical synthesis*
D019151:Peptide Library; D010455:Peptides