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Development of Aminoglycoside Based HIV Therapeutics

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: 1 R43 AI38734-01,
Agency Tracking Number: 29149
Amount: $100,000.00
Phase: Phase I
Program: SBIR
Solicitation Topic Code: N/A
Solicitation Number: N/A
Solicitation Year: N/A
Award Year: 1995
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
200 Boston Avenue, Suite 3000
Medford, MA 02155
United States
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 Mark Wuonola
 () -
Business Contact
Phone: () -
Research Institution

The goal of this research is to synthesize orally active derivatives of a lead compound, neomycin Breplication of the AIDS virus at the level of transcription by inhibiting the Rev protein/RRE interabetween this protein and sequence of nucleic acid is crucial to the virus life cycle. Recent work hasmall molecule antibiotic neomycin B is capable of disrupting the binding of Rev to the RRE. Such aneffective therapeutic for HIV. However, neomycin B needs improvement in such areas as its cytotoxicispecificity for the Rev/RRE interaction. Also, syntheses of the large number of compounds necessarywould be time consuming and difficult using existing literature methods due to the highly functionalof the lead compound. We will approach this problem by the production of appropriately protected syncommercially available ribostamycin as a starting material. This approach will allow one to produceneomycin analogs expediently by appending D-ring analogs of wide functional and structural diversitymultiple assays exist in house to provide activity data on all analogs.

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

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