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NUCLEOSIDE PHOSPHATE ANALOGUES WITH BORONATED PHOSPHATES

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
16296
Program Year/Program:
1993 / SBIR
Agency Tracking Number:
16296
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
BORON BIOLOGICALS, INC.
620 HUTTON ST, STE 104 RALEIGH, NC 27606
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Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 2
Fiscal Year: 1993
Title: NUCLEOSIDE PHOSPHATE ANALOGUES WITH BORONATED PHOSPHATES
Agency: HHS
Contract: N/A
Award Amount: $483,092.00
 

Abstract:

USE OF NUCLEOSIDE PHOSPHATES AS ANTITUMOR AND ANTIVIRAL AGENTS HAS BEEN LIMITED BY THEIR INABILITY TO PENETRATE CELL MEMBRANES AS WELL AS THEIR HIGH SUSCEPTIBILITY TO ENZYMES SUCH AS PHOSPHATASES, NUCLEOTIDASES, ETC. MODIFICATION OF THE PHOSPHATE GROUP (BY REPLACING ONE OF THE NONBRIDGING OXYGENS WITH A BORANE GROUP) MAY PROVIDE BOTH THE MEMBRANE PERMEABILITY TO THESE COMPOUNDS AND THE STABILITY (TOWARDS PHOSPHATE-REMOVING ENZYMES). THE LONG- TERM OBJECTIVE OF THIS PROJECT IS TO SYNTHESIZE NUCLEOSIDE MONO-, DI- AND TRIPHOSPHATES IN WHICH ONE OF THE OXYGENS OF \, A OR G PHOSPHORUS HAS BEEN REPLACED WITH AN ISOELECTRONIC BORANE GROUP. THESE COMPOUNDS MAY BE PREPARED BY PHOSPHORYLATION OF NUCLEOSIDES, NUCLEOSIDE MONOPHOSPHATES AND NUCLEOSIDE DIPHOSPHATES USING A BORONATED PHOSPHORYLATING AGENT. IN OUR STUDIES WITH RELATED OLIGONUCLEOTIDE BORANOPHOSPHATES, THE P-BH3 MOIETY HAS BEEN FOUND TO BE REMARKABLY STABLE AND THE OLIGONUCLEOTIDE BORANOPHOSPHATES HAVE HIGH NUCLEASE RESISTANCE. THE NUCLEOSIDE BORANOPHOSPHATES MAY BE USEFUL IN A NUMBER OF WAYS INCLUDING: 1) AS TOOLS FOR STUDYING MECHANISM OF ACTION OF ENZYMES, 2) AS ANTIVIRAL AND ANTITUMOR AGENTS, AND 3) AS CARRIERS OF BORON FOR BORON NEUTRON CAPTURE THERAPY.

Principal Investigator:

Spielvogel, Bernard F
Principal Investigator
9198322044

Business Contact:

1 r43 ai30887-01
Small Business Information at Submission:

Boron Biologicals, Inc.
533 Pylon Drive P O Box 3348 9 Raleigh, NC 27636

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