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EBI PDBe PDBeView

PDBe Entry: 1tl8 view

Human DNA topoisomerase I (70 kDa) in complex with the indenoisoquinoline AI-III-52 and covalent complex with a 22 base pair DNA duplex
Summary
Header ISOMERASE/DNAsearch
Method X-RAY DIFFRACTION
Experiment Resolution: 3.1 Å, R-factor: 22.9%, Free R-factor: 30.5%, Spacegroup: P 1 21 1
Released 21/06/2005, deposition: 09/06/2004, last revision: 24/02/2009
Authors Ioanoviciu, A.search; Antony, S.search; Pommier, Y.search; Staker, B.L.search; Stewart, L.search; Cushman, M.search
Primary citation Synthesis 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
J.MED.CHEM.search vol:48, pag:4803-4814 (2005) [PubMed ID 16033260 ]search
Keywords COMPLEX (ISOMERASE/DNA)search, DNAsearch, TOPOISOMERASE Isearch, DRUGsearch, POISONsearch, IDENOISOQUINOLINEsearch
EC 5.99.1.2 ExPASy BRENDA search (A)
Organism Homo sapiens(human) 9606search(A)
UniProt DNA topoisomerase 1 (EC 5.99.1.2) (DNA topoisomerase I) P11387search (A)
Related entries 1k4t
Polymers
Id Name Type UniProt Residues Observed
B 5'-D(*AP*AP*AP*AP*AP*GP*AP*CP*TP*T)-3' DNA
10 100%
C 5'-D(*(TPC)P*GP*AP*AP*AP*AP*AP*TP*TP*TP*TP*T)-3' DNA
12 100%
D 5'-D(*AP*AP*AP*AP*AP*TP*TP*TP*TP*TP*CP*GP*AP*AP*GP*TP*CP*TP*TP*TP*TP*T)-3' DNA
22 100%
A DNA topoisomerase I Protein P11387 (TOP1_HUMAN)search
 592 95%
Heterogens
Id Name Ligands
D 2,3-DIMETHOXY-12H-[1,3]DIOXOLO[5,6]INDENO[1,2-C]ISOQUINOLIN-6-IUM AI3 search
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