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Abstract

Grant Number: 1R43CA096484-01
PI Name: DENG, JING-ZHEN
PI Email:
PI Title: SENIOR SCIENTIST
Project Title: Potentiation of Topoisomerase I Inhibitors

Abstract: DESCRIPTION (provided by applicant): The overall goal of this SBIR is the identification of small molecules that can reinforce the antitumor activity of DNA topoisomerase I inhibitors by acting at a biochemical locus linked functionally to topoisomerase I. This is to be done by selecting natural products from plant and marine extracts that inhibit the topoisomerase I-linked locus, and then modifying the structures of the isolated active principles. The compounds so identified will be evaluated in cell free systems, and in suitable yeast tester strains and mammalian cell lines. Optimized inhibitors will be evaluated in suitable animal tumor models as potentiators of the activity of DNA topoisomerase I inhibitors. PROPOSED COMMERCIAL APPLICATION: The goal of this program is the identification and commercialization of agents that can potentiate the activity of topisomerase I inhibitors as antitumor agents. The annual market for an agents. The annual market for an agent of this type should be well in excess of $100 million.

Thesaurus Terms:
DNA topoisomerase, antineoplastic, biological product, biological response modifier, drug design /synthesis /production, enzyme inhibitor
drug discovery /isolation, method development
cell free system, tissue /cell culture, yeast

Institution: PINNACLE PHARMACEUTICALS
MC CORMICK RD/UVA CHEMISTRY BLDG
CHARLOTTESVILLE, VA 22903
Fiscal Year: 2002
Department:
Project Start: 01-APR-2002
Project End: 31-DEC-2003
ICD: NATIONAL CANCER INSTITUTE
IRG: ZRG1


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