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Generic Fluorescent HTS Assay for Oxidoreductases

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
89180
Program Year/Program:
2008 / SBIR
Agency Tracking Number:
GM083478
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
BELLBROOK LABS, LLC
5500 NOBEL DR, STE 230 MADISON, WI -
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2008
Title: Generic Fluorescent HTS Assay for Oxidoreductases
Agency: HHS
Contract: 1R43GM083478-01
Award Amount: $210,100.00
 

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.

Principal Investigator:

Robert G. Lowery
6082274501
BOB.LOWERY@BELLBROOK-LABS.COM

Business Contact:


bob.lowery@bellbrooklabs.com
Small Business Information at Submission:

BELLBROOK LABS, LLC
5500 Nobel Drive Suite 250 MADISON, WI 53711

EIN/Tax ID: 043661356
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No