Hanlin Gao, E. Yamasaki, K. Chan
Nov 1, 2000
Citations
0
Influential Citations
34
Citations
Journal
Cancer Research
Abstract
Chloroquinoxaline sulfonamide (chlorosulfaquinoxaline, CQS, NSC 339004) is active against murine and human solid tumors. On the basis of its structural similarity to the topoisomerase IIβ-specific drug XK469, CQS was tested and found to be both a topoisomerase-IIα and a topoisomerase-IIβ poison. Topoisomerase II poisoning by CQS is essentially undetectable in assays using the common protein denaturant SDS, but easily detectable with strong chaotropic protein denaturants. The finding that detection of topoisomerase poisoning can be so dependent on the protein denaturant used in the assay has implications for drug discovery efforts and for our understanding of topoisomerase poisons.