Abstract: This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
Type:
Grant
Filed:
May 8, 2014
Date of Patent:
July 19, 2016
Assignee:
The University of Denver and Regis University
Inventors:
Scott Dusan Pegan, Kateri Ahrendt, Glenn C. Capodagli, Bryan Cowen
Abstract: This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
Type:
Application
Filed:
May 8, 2014
Publication date:
November 13, 2014
Applicants:
Colorado Seminary, Which Owns and Operates The University Of Denver, Regis University
Inventors:
Scott Dusan Pegan, Kateri Ahrendt, Glenn C. Capodagli, Bryan Cowen