Chimmitecan is a novel lipophilic camptothecin derivative with improved anticancer pharmacologic profiles compared with the clinical available analogs. Chimmitecan directly interacts with the topoisomerase I-DNA complex, characterized by its outstanding binding affinity. The most probable binding conformation of chimmitecan to the cleavable complex was predicted by automated molecular docking based on the X-ray crystal structure of the toposiomerase I-DNA complex, with topoisomerase I in blue and DNA helices in orange. Residues colored purple represent hydrophobicinteraction with the compound and dash line represents hydrogen bond between chimmitecan and topoisomerase I. For further details, please see Huang et al. on page 1298 in this issue.

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