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TitleSynthesis and Mechanism of Action Studies of a Series of Norindenoisoquinoline Topoisomerase I Poisons Reveal an Inhibitor with a Flipped Orientation in the Ternary DNA-Enzyme-Inhibitor Complex As Determined by X-ray Crystallographic Analysis
Journal, issue, pagesJ. Med. Chem., Vol. 48, Page 4803-4814, Year 2005
Publish dateJun 9, 2004 (structure data deposition date)
AuthorsIoanoviciu, A. / Antony, S. / Pommier, Y. / Staker, B.L. / Stewart, L. / Cushman, M.
External linksJ. Med. Chem. / PubMed:16033260
MethodsX-ray diffraction
Resolution3.1 Å
Structure data

PDB-1tl8:
Human DNA topoisomerase I (70 kDa) in complex with the indenoisoquinoline AI-III-52 and covalent complex with a 22 base pair DNA duplex
Method: X-RAY DIFFRACTION / Resolution: 3.1 Å

Chemicals

ChemComp-AI3:
2,3-DIMETHOXY-12H-[1,3]DIOXOLO[5,6]INDENO[1,2-C]ISOQUINOLIN-6-IUM

Source
  • homo sapiens (human)
KeywordsISOMERASE/DNA / COMPLEX (ISOMERASE-DNA) / DNA / TOPOISOMERASE I / DRUG / POISON / IDENOISOQUINOLINE / ISOMERASE-DNA complex

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