Staff Publications

Staff Publications

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    'Staff publications' is the digital repository of Wageningen University & Research

    'Staff publications' contains references to publications authored by Wageningen University staff from 1976 onward.

    Publications authored by the staff of the Research Institutes are available from 1995 onwards.

    Full text documents are added when available. The database is updated daily and currently holds about 240,000 items, of which 72,000 in open access.

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Record number 496396
Title Involvement of a Hydrophobic Pocket and Helix 11 in Determining the Modes of Action of Prenylated Flavonoids and Isoflavonoids in the Human Estrogen Receptor
Author(s) Schans, M.G.M. van de; Ritschel, T.; Bovee, T.F.H.; Sanders, M.G.; Waard, P. de; Gruppen, H.; Vincken, J.P.
Source ChemBioChem 16 (2015)18. - ISSN 1439-4227 - p. 2668 - 2677.
DOI https://doi.org/10.1002/cbic.201500343
Department(s) Food Chemistry Group
RIKILT - BU Toxicology Bioassays & Novel Foods
BioNanoTechnology
ATV NMR Centrum
VLAG
Publication type Refereed Article in a scientific journal
Publication year 2015
Abstract Six prenylated (iso)flavonoids were purified from a licorice root extract and subjected to competition experiments with six commercially available (iso)flavonoids. The agonistic and antagonistic activities of these compounds towards both hERa (human estrogen receptor alpha) and hERb were determined. Differences in the modes of action (agonist or antagonist) were observed for the various compounds tested. In general, each compound had the same mode of action towards both ERs. In silico modeling was performed in order to study the differences in estrogenicity observed between the compounds. It is suggested that prenyl chains fit into a hydrophobic pocket present in the hER, resulting in an increased agonistic activity. In addition, it was shown that an increase in length (…1.7 æ) of pyran prenylated isoflavonoids resulted in an antagonistic mode of action. This might be caused by collision of the pyran ring with helix 11 in the ligand binding cavity of the hER.
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