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=== '''Human topoisomerase IIbeta in complex with DNA and etoposide''' ===
=== '''Human topoisomerase IIbeta in complex with DNA and etoposide''' ===
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<Structure load='3qx3' size='600' frame='true' align='right' caption='Insert caption here' scene='Insert optional scene name here' /><!-- PLEASE DO NOT DELETE THIS TEMPLATE -->
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Crystal structure of a large fragment of human type II topoisomerases (TOP2) complexed to DNA and to the anticancer drug etoposide to reveal structural details of drug-induced stabilization of a cleavage complex<ref>PMID: 21778401</ref>.  
Crystal structure of a large fragment of human type II topoisomerases (TOP2) complexed to DNA and to the anticancer drug etoposide to reveal structural details of drug-induced stabilization of a cleavage complex<ref>PMID: 21778401</ref>.  

Revision as of 17:29, 19 September 2012

Human topoisomerase IIbeta in complex with DNA and etoposide

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Crystal structure of a large fragment of human type II topoisomerases (TOP2) complexed to DNA and to the anticancer drug etoposide to reveal structural details of drug-induced stabilization of a cleavage complex[1].

The interplay between the protein, the DNA, and the drug explains the structure-activity relations of etoposide derivatives and the molecular basis of drug-resistant mutations.

Also, at the active site we can see the ligand, and both alpha helices, and beta sheets at the secondary structures.

References

  1. ↑ Wu CC, Li TK, Farh L, Lin LY, Lin TS, Yu YJ, Yen TJ, Chiang CW, Chan NL. Structural basis of type II topoisomerase inhibition by the anticancer drug etoposide. Science. 2011 Jul 22;333(6041):459-62. PMID:21778401 doi:10.1126/science.1204117