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Technology for isolation of Integrase Inhibitors for Therapeutics against Human…

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
93457
Program Year/Program:
2009 / SBIR
Agency Tracking Number:
AI084610
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
INTEGRATECH PROTEOMICS, INC.
615 ARAPEEN DR. SALT LAKE CITY, UT 84108
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2009
Title: Technology for isolation of Integrase Inhibitors for Therapeutics against Human I
Agency: HHS
Contract: 1R43AI084610-01
Award Amount: $599,602.00
 

Abstract:

DESCRIPTION (provided by applicant): Currently there are 40 million people estimated to be infected with HIV/AIDS worldwide; 22 million people have died since its discovery in 1980's. Drugs inhibiting the reverse transcriptase (RT), protease, and integrase - three essential enzymes for the replication and propagation of HIV in the host - are available. However, viral resistance and drug side effects necessitate development of new treatments for HIV/AIDS. One target among these three may prove to have furthe r drugable domains. Although in vitro screens for inhibitory drugs against HIV integrase (INT) have been difficult due to its low aqueous solubility and propensity toward protein aggregation, we have discovered an inhibitory peptide against INT using a y east two hybrid assay. The peptide has a unique mode of action than the current strand transfer inhibitors. This inhibitory peptide in conjunction with yeast two hybrid technology may lend itself to a screening platform resulting in the discovery of novel inhibitory compounds of INT. The goal of the proposed research is to obtain a small molecule that mimics the mechanistic effects of a peptide inhibitor of HIV INT. Briefly, the specific aims are 1) to optimize target-peptide displacement assays; 2) to scre en chemical libraries under high throughput conditions for compounds that disrupt peptide-HIV INT interaction in yeast; and 3) to select the best candidates for screening. PUBLIC HEALTH RELEVANCE: The proposed research describes methods to isolate novel dr ugs that inhibit HIV integrase, an essential enzyme in the replication cycle of this devastating virus. Compounds isolated that possess desirable inhibitory properties will be optimized for further pre-clinical studies.

Principal Investigator:

Tanya M. Sandrock
8015832787
TANYA.SANDROCK@ARUPLAB.COM

Business Contact:

Danuta Petelenx
Small Business Information at Submission:

INTEGRATECH PROTEOMICS, INC.
615 ARAPEEN DR. SALT LAKE CITY, UT 84108

EIN/Tax ID: 180031035
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No