Patent Number: 6,309,881

Title: Antibody catalysis of enantio- and diastereo-selective aldol reactions

Abstract: Nine efficient aldolase antibodies were generated using hapten 2. This hapten combines, in a single molecule, structural components employed for reactive immunization with structural components employed for forming a transition state analog of the aldol reaction. Characterization of two of these antibodies reveals that they are highly proficient (up to 1000-fold better than any other antibody catalyst) and enantioselective catalysts for aldol and retro-aldol reactions and exhibit enantio- and diastereo-selectivities opposite that of antibody 38C2.

Inventors: Barbas; Carlos F. (Del Mar, CA), Lerner; Richard A. (La Jolla, CA), Zhong; Guofu (San Diego, CA)

Assignee: The Scripps Research Institute

International Classification: C07D 277/24 (20060101); C07D 277/36 (20060101); C07D 277/34 (20060101); C07D 417/06 (20060101); C07D 277/00 (20060101); C07D 417/00 (20060101); C07D 493/04 (20060101); C07D 493/00 (20060101); C12P 17/18 (20060101); C12P 17/16 (20060101); C12P 41/00 (20060101); C12P 7/24 (20060101); C12P 7/26 (20060101); C12N 9/00 (20060101); C12N 005/12 ()

Expiration Date: 10/30/2018