Structure of PDB 1sc7 Chain A Binding Site BS01

Receptor Information

>1sc7 Chain A (length=567) Species: 9606 (Homo sapiens)

EEQKWKWWEEERYPEGIKWKFLEHKGPVFAPPYEPLPENVKFYYDGKVMK
LSPKAEEVATFFAKMLDHEYTTKEIFRKNFFKDWRKEMTNEEKNIITNLS
KCDFTQMSQYFKAQTEARKQMSKEEKLKIKEENEKLLKEYGFCIMDNHKE
RIANFKIEPPGLFRGRGNHPKMGMLKRRIMPEDIIINCSKDAKVPSPPPG
HKWKEVRHDNKVTWLVSWTENIQGSIKYIMLNPSSRIKGEKDWQKYETAR
RLKKCVDKIRNQYREDWKSKEMKVRQRAVALYFIDKLALRAGNEKEEGET
ADTVGCCSLRVEHINLHPELDGQEYVVEFDFLGKDSIRYYNKVPVEKRVF
KNLQLFMENKQPEDDLFDRLNTGILNKHLQDLMEGLTAKVFRTYNASITL
QQQLKELTAPDENIPAKILSYNRANRAVAILCNHQRAPPKTFEKSMMNLQ
TKIDAKKEQLADARRDLKSAKADAKVMKDAKTKKVVESKKKAVQRLEEQL
MKLEVQATDREENKQIALGTSKLNYLDPRITVAWCKKWGVPIEKIYNKTQ
REKFAWAIDMADEDYEF

Ligand information

>1sc7 Chain B (length=10)

aaaaagactt

Receptor-Ligand Complex Structure

Structure summary

• PDB: 1sc7 Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex
• Resolution: 3.0 Å
• Binding residue (original residue number in PDB): V410 T411 W412 I424 Y426 M428 K436 K439 K443 N722 Y723
• Binding residue (residue number reindexed from 1): V212 T213 W214 I226 Y228 M230 K238 K241 K245 N524 Y525
• Binding affinity: PDBbind-CN: IC50=4.9uM

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

External links

• PDB: RCSB:1sc7, PDBe:1sc7, PDBj:1sc7
• PDBsum: 1sc7
• PubMed: 15801827
• UniProt: P11387|TOP1_HUMAN DNA topoisomerase 1 (Gene Name=TOP1)