Rational Inhibitors of DNA Base Excision (BER) Enzymes: New Tools for Elucidating the Role of BER in Cancer Chemotherapy
Abstract
In this funding period we have completed Task 1 of the approved Statement of Work which seeks to develop useful inhibitor scaffolds for the DNA repair enzyme uracil DNA glycosylase (UDG). In addition, we have performed groundbreaking studies that shed light on the molecular basis of substrate recognition by UDG. These new studies provide exciting avenues for rational inhibitor development with potential for anticancer therapy. Major findings in this period include the synthesis and screening of new bipartite transition state-based inhibitors for UDG, and the exploration of the roles of hydrogen bonding and molecular flexibility in specific recognition by the enzyme. This work has resulted in two publications during this period.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 2004
- Accession Number
- ADA424155
Entities
People
- Daniel J. Krosky
- James T. Stivers
Organizations
- Johns Hopkins University