Wisconsin Alumni Research Foundation

William Seth Horne

Samuel Helmer Gellman

Lisa M Johnson

Li Guo

Yonggui Chi

William C Pomerantz

Emily P English

Described is a method of fabricating biologically active, unnatural polypeptides. The method includes the steps of selecting a biologically active polypeptide or biologically active fragment thereof having an amino acid sequence comprising &#x3b1;-amino acid residues, and fabricating a synthetic polypeptide that has an amino acid sequence that corresponds to the sequence of the biologically active polypeptide, but wherein about 14% to about 50% of the &#x3b1;-amino acid residues found in the biologically active polypeptide or fragment of step (a) are replaced with &#x3b2;-amino acid residues, and the &#x3b1;-amino acid residues are distributed in a repeating pattern.

Method of making biologically active alpha-beta peptides

The present invention provides a method for the synthesis of &#x3b2;-amino acids. The method also provides methods yielding &#x3b1;-substituted &#x3b2;-amino aldehydes and &#x3b2;-substituted &#x3b3;-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of &#x3b2;-amino acids.

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Madison, WI, United States of America

William Seth Horne