Topoisomerases are nuclear enzymes that play an essential role in DNA metabolism and have emerged as the receptors for several clinically important anticancer agents. This proposal describes a research program directed toward the chemistry and biology of two classes of natural products that exhibit excellent antitumor activity by """"""""poisoning"""""""" topoisomerase II. With a combination of bioorganic, computational and biological studies we aim to elucidate the mode of action of the above compounds and address issues pertaining to their structure-activity relationship. Research along these lines is expected to aid in the development of powerful and selective anticancer agents and could have important implications for cancer treatment.

Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Research Project (R01)
Project #
5R01CA085600-03
Application #
6628456
Study Section
Bio-Organic and Natural Products Chemistry Study Section (BNP)
Program Officer
Fu, Yali
Project Start
2001-02-02
Project End
2005-01-31
Budget Start
2003-02-01
Budget End
2004-01-31
Support Year
3
Fiscal Year
2003
Total Cost
$198,394
Indirect Cost
Name
University of California San Diego
Department
Chemistry
Type
Schools of Arts and Sciences
DUNS #
804355790
City
La Jolla
State
CA
Country
United States
Zip Code
92093
Haidekker, Mark A; Brady, Thomas; Wen, Ke et al. (2002) Phospholipid-bound molecular rotors: synthesis and characterization. Bioorg Med Chem 10:3627-36