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Generic Fluorescent HTS Assay for Oxidoreductases

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: 1R43GM083478-01
Agency Tracking Number: GM083478
Amount: $210,100.00
Phase: Phase I
Program: SBIR
Solicitation Topic Code: N/A
Solicitation Number: PHS2007-2
Timeline
Solicitation Year: 2008
Award Year: 2008
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
5500 Nobel Drive Suite 250
MADISON, WI 53711
United States
DUNS: 119165251
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 ROBERT LOWERY
 (608) 227-4501
 BOB.LOWERY@BELLBROOK-LABS.COM
Business Contact
Phone: (608) 227-4501
Email: bob.lowery@bellbrooklabs.com
Research Institution
N/A
Abstract

DESCRIPTION (provided by applicant): There is a high level of pharmaceutical interest in targeting enzymes that catalyze oxidation and reduction reactions for therapeutic intervention. Validated redox enzyme targets include HMG-CoA reductase, the target of
statin drugs like Lipitor that are used to treat hypercholesterolemia, and 51-reductase, the target of drugs used to treat benign prostatic hyperdysplasia. Emerging targets in this class include glycolytic dehydrogenases in tumor cells growing under hypox
ic conditions and in microbial and parasitic pathogens. However, the identification of novel inhibitors for redox enzymes is being slowed by the lack of robust, generic enzyme assay methods that are suitable for use in pharmaceutical high throughput screen
ing (HTS) laboratories. To remove this technical hurdle, we are proposing to develop methods for specific, fluorescent detection of oxidized and reduced pyridine nucleotides, NAD(H) and NADP(H). Methods will be developed for specific chemical modification
of pyridine nucleotides based on their oxidation state. Comcomitantly, antibodies and fluorescent tracers will be developed for homogenous immunodetection of unmodified pyridine nucleotides. These novel reagents and methods will be validated for homogenous
detection of dehydrogenase and reductase enzyme activity in a fluorescence polarization immunoassay format and commercialized as HTS assay kits. The availability of robust, fluorescence based assay methods applicable to any redox enzyme that utilizes a py
ridine nucleotide cofactor will accelerate the exploration of this validated target class for a broad range of diseases and disorders. Enzymes that catalyze oxidation and reduction reactions constitute a major class of proteins that have been succes
sfully exploited as drug targets. We are proposing to develop methods and reagents that will enable pharmaceutical researchers to accelerate drug discovery targeting these enzymes for a broad range of diseases including cancer, cardiovascular disease, and
diabetes.

* Information listed above is at the time of submission. *

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