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Constrained phytoestrogens and analogues as ERβ selective ligands by Chris P Miller; Michael D Collini; Heather A Harris is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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A new series of ERbeta (ERbeta) selective ligands has been prepared. One of the compounds 6, structurally related to the phytoestrogen apigenin 4, displays a binding preference for ERbeta over ERalpha of over 40-fold. In addition to its binding selectivity, 6 was able to potently induce metallothionein (an ERbeta specific response in human SAOS-2 cells) while demonstrating low potency in an ERalpha dependant ERE-tk luciferase assay in MCF-7 cells. Such receptor and cell selectivity could make 6 a useful molecular probe for better understanding the role of ERbeta in mammalian physiology.

Who reads Constrained phytoestrogens and analogues as ERβ selective ligands?

Author

Chris P Miller; Michael D Collini; Heather A Harris

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2003

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)