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Activated Sugars for Drug Discovery

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
80094
Program Year/Program:
2009 / SBIR
Agency Tracking Number:
GM079004
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
ZUCHEM, INC.
2225 W. Harrison St. CHICAGO, IL 60612-4671
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 2
Fiscal Year: 2009
Title: Activated Sugars for Drug Discovery
Agency: HHS
Contract: 2R44GM079004-02A1
Award Amount: $773,902.00
 

Abstract:

DESCRIPTION (provided by applicant): The overall goal of this proposal is to create a robust one pot, in vitro, multi-gram scale synthesis of activated sugars for drug discovery and biochemical research purposes. Natural product glycosylation is vital for the discovery of new pharmaceutical compounds. While it has been recognized for some time that many biologically active natural products owe much of their therapeutic properties to their glycosylation diversity, methods for creating further diversity for d rug discovery have been difficult to develop. One of the challenges is that the modified and rare sugars needed for creating diversity are unavailable or extremely difficult to make, and that the sugars need to be chemically activated in order to transfe r them to the core natural product molecule. However, new technology has been developed where a chemoenzymatic method is used to attach sugars to natural production aglycons. With this method, a combination of a kinase and nucleotide transferase are needed to form the specific activated sugar and finally a glycosyltransferase is used to transfer the sugar to an appropriate aglycon core. This technology is valuable for drug discovery, as it can be used to produce a library of differentially glycosylated natu ral product molecules. The Phase II research of this project will continue the improvements in the enzymes needed for this process, including engineering a greater substrate range. The research will then focus on coupling the best enzymes, ATP/NTP regenera tion, product recovery, process scale-up and creating novel antibiotic derivatives as a demonstration of the developed technology. PUBLIC HEALTH RELEVANCE: This project is aimed toward developing a method for making a variety of activated sugars for drug d iscovery purposes. These sugars can used to make derivatives of natural products with new therapeutic properties, for example, antibiotics that are effective against antibiotic-resistant bacteria.

Principal Investigator:

Ryan Woodyer
3129972150
RWOODYER@ZUCHEM.COM

Business Contact:

Gina Berardesco
ginab@zuchem.com
Small Business Information at Submission:

ZUCHEM, INC.
ZUCHEM, INC. 2225 W. Harrison St. CHICAGO, IL 60612

EIN/Tax ID: 311814959
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No