Topoisomerase targeted agents - chemistry to chemotherapy

This meeting demonstrated the extent of new knowledge on the interaction of topoisomerase enzymes with DNA at the molecular level, including their high level of sequence recognition and their efficient DNA cleavage and religation mechanisms. Speakers discussed the use of this new knowledge to create detailed models of enzyme/DNA/drug ternary complexes, and to design more efficient enzyme inhibitors. Other factors needed to turn an efficient inhibitor into a useful drug were also reported on; these included selectivity, distribution, metabolism, macromolecular binding, scheduling and toxicity profiles.