Structure of PDB 1t8i Chain A Binding Site BS03

Receptor Information
>1t8i Chain A (length=565) Species: 9606 (Homo sapiens) [Search protein sequence] [Download receptor structure] [Download structure with residue number starting from 1] [View receptor structure]
QKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKFYYDGKVMKLS
PKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLSKC
DFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKERI
ANFKIEPPGLFRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPGHK
WKEVRHDNKVTWLVSWTENIQGSIKYIMLNPSSRIKGEKDWQKYETARRL
KKCVDKIRNQYREDWKSKEMKVRQRAVALYFIDKLALRAGNEKEEGETAD
TVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNKVPVEKRVFKN
LQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITLQQ
QLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQTK
IDAKKEQLADARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQLMK
LEVQATDREENKQIALGTSKLNYLDPRITVAWCKKWGVPIEKIYNKTQRE
KFAWAIDMADEDYEF
Ligand information
Receptor-Ligand Complex Structure
Global viewLocal viewStructure summary

[Spin on] [Spin off] [Reset]
[High quality] [Low quality]
[White background] [Black background]
[Spin on] [Spin off] [Reset]
[High quality] [Low quality]
[White background] [Black background]
PDB1t8i Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex
Resolution3.0 Å
Binding residue
(original residue number in PDB)		E356 F361 R362 G363 R364 H367 K374 R488 A489 N491 K493 T501 K532 D533 N574 T585 A586 K587 N646
Binding residue
(residue number reindexed from 1)		E156 F161 R162 G163 R164 H167 K174 R288 A289 N291 K293 T301 K332 D333 N374 T385 A386 K387 N446
Binding affinityPDBbind-CN: IC50=0.3uM
Enzymatic activity
Enzyme Commision number 5.6.2.1: DNA topoisomerase.
Gene Ontology
Molecular Function
GO:0003677 DNA binding
GO:0003917 DNA topoisomerase type I (single strand cut, ATP-independent) activity
Biological Process
GO:0006265 DNA topological change
Cellular Component
GO:0005694 chromosome

View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB RCSB:1t8i, PDBe:1t8i, PDBj:1t8i
PDBsum1t8i
PubMed15801827
UniProtP11387|TOP1_HUMAN DNA topoisomerase 1 (Gene Name=TOP1)

[Back to BioLiP]