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DNA‐Controlled Bivalent Presentation of Ligands for the Estrogen Receptor
Author(s) -
Abendroth Frank,
Bujotzek Alexander,
Shan Min,
Haag Rainer,
Weber Marcus,
Seitz Oliver
Publication year - 2011
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201101655
Subject(s) - bivalent (engine) , estrogen receptor , dna , chemistry , conjugated system , presentation (obstetrics) , computational biology , biochemistry , combinatorial chemistry , stereochemistry , biology , genetics , medicine , breast cancer , organic chemistry , polymer , radiology , cancer , metal
Molecular ruler : Steroid analogues were conjugated to DNA by using click chemistry, and self‐assembly provided ternary DNA complexes with bivalent ligand presentation. The distance between the bound ligands was measured by spatial screening of the estrogen receptor, and a second hydrophobic binding site was postulated. The picture shows the DNA(black)–raloxifene(orange) complex in the ligand binding domain of the receptor.