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Hormone–PAMAM Dendrimer Conjugates: Polymer Dynamics and Tether Structure Affect Ligand Access to Receptors
Author(s) -
Kim Sung Hoon,
Katzenellenbogen John A.
Publication year - 2006
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.200601923
Subject(s) - dendrimer , receptor , estrogen receptor , hormone receptor , chemistry , conjugate , ligand (biochemistry) , conjugated system , biophysics , polymer , biochemistry , medicine , biology , breast cancer , mathematics , organic chemistry , cancer , mathematical analysis
An open and closed case : Estradiol was conjugated to a PAMAM dendrimer (gray circle) through a short (17α‐phenylethynyl) or a long (hexaethyleneglycol) tether to evaluate how ligand access to a receptor is affected. With the short tether (a), the hormone is free and solvent exposed, with unimpeded access to the estrogen receptor, while the long tether (b) wraps around the hormone and the dendrimer and markedly reduces access to the receptor.