Eur J Cancer. 2000 Sep;36 Suppl 4:S34-5.

Modulation of oestrogen action by receptor gene inhibition.

Madden TA, Barrow D, McClelland RA, Gee JM, Nicholson RI.

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Tenovus Cancer Research Centre, Welsh School of Pharmacy, Redwood Building, King Edward VII Ave, CF10 3XE, Cardiff, UK. maddenta1@cardiff.ac.uk

Abstract

Selective oestrogen receptor downregulators (SERDs) are a class of highly effective steroidal antitumour agents that reduce cellular levels of the oestrogen receptor (ER). In this study, we compared the efficacy by which three novel molecular approaches: (1) antisense oligonucleotides; (2) antisense RNA; and (3) dominant negative mutants are able to act as SERDs. Using transient and, where appropriate, stable gene transfection experiments we found that constitutive overexpression of ER antisense RNA and a hormone-binding domain compromised dominant-negative ER mutant (DNER-1), were most effective at downregulating ER expression and/or activity in vitro.

PMID:: 11056309; [PubMed - indexed for MEDLINE]

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