Technology for isolation of Integrase Inhibitors for Therapeutics against Human I

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$599,602.00
Award Year:
2009
Program:
SBIR
Phase:
Phase I
Contract:
1R43AI084610-01
Award Id:
93457
Agency Tracking Number:
AI084610
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
615 ARAPEEN DR., SALT LAKE CITY, UT, 84108
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
828972765
Principal Investigator:
TANYASANDROCK
(801) 583-2787
TANYA.SANDROCK@ARUPLAB.COM
Business Contact:
DANUTAPETELENX
() -
Research Institute:
n/a
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.

* information listed above is at the time of submission.

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