Article
A structural model for the ternary cleavable complex formed between human topoisomerase I, DNA, and camptothecin.
Biochemistry - 21 Aug 2001
Kerrigan J E, Pilch D S
Abstract excerpt
Using the X-ray crystal structure of the human topoisomerase I (TOP1)-DNA cleavable complex, we have developed a general model for the ternary drug-DNA-TOP1 cleavable complex formed with camptothecin (CPT) and its analogues. This model has the drug intercalated between the -1 and +1 base pairs, with the E-ring pointing into the minor groove and the A-ring directed toward the major groove. The ternary complex is...
Topics
- Antineoplastic Agents, Phytogenic
- Base Sequence
- Camptothecin
- Computer Simulation
- Cross-Linking Reagents
- DNA
- DNA Topoisomerases, Type I
- Enzyme Inhibitors
- Humans
- Kinetics
- Models, Chemical
- Models, Molecular
- Molecular Sequence Data
- Mutation
- Protein Binding