Development of subtype-selective oestrogen receptor-based therapeutics

Stefan Nilsson; Konrad F. Koehler; Jan Åke Gustafsson

doi:10.1038/nrd3551

Development of subtype-selective oestrogen receptor-based therapeutics

Stefan Nilsson, Konrad F. Koehler, Jan Åke Gustafsson

Research output: Contribution to journal › Review article › peer-review

223 Scopus citations

Abstract

The two oestrogen receptor subtypes α and β are hormone-regulated modulators of intracellular signalling and gene expression. Regulation of oestrogen receptor activity is crucial not only for development and homeostasis but also for the treatment of various diseases and symptoms. Classical selective oestrogen receptor modulators are well established in the treatment of breast cancer and osteoporosis, but emerging data suggest that the development of subtype-selective ligands that specifically target either oestrogen receptor-α or oestrogen receptor-β could be a more optimal approach for the treatment of cancer, cardiovascular disease, multiple sclerosis and Alzheimer's disease.

Original language	English (US)
Pages (from-to)	778-792
Number of pages	15
Journal	Nature Reviews Drug Discovery
Volume	10
Issue number	10
DOIs	https://doi.org/10.1038/nrd3551
State	Published - Oct 2011

ASJC Scopus subject areas

Pharmacology
Drug Discovery

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10.1038/nrd3551

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title = "Development of subtype-selective oestrogen receptor-based therapeutics",

abstract = "The two oestrogen receptor subtypes α and β are hormone-regulated modulators of intracellular signalling and gene expression. Regulation of oestrogen receptor activity is crucial not only for development and homeostasis but also for the treatment of various diseases and symptoms. Classical selective oestrogen receptor modulators are well established in the treatment of breast cancer and osteoporosis, but emerging data suggest that the development of subtype-selective ligands that specifically target either oestrogen receptor-α or oestrogen receptor-β could be a more optimal approach for the treatment of cancer, cardiovascular disease, multiple sclerosis and Alzheimer's disease.",

author = "Stefan Nilsson and Koehler, {Konrad F.} and Gustafsson, {Jan {\AA}ke}",

note = "Funding Information: Research in J.-{\AA}.G{\textquoteright}s laboratory is supported by The Swedish Cancer Fund, the Welch Foundation (Houston, Texas, USA) and the Texas Emerging Technology Fund (Austin, Texas, USA) under agreement number 300-9-1958. Copyright: Copyright 2012 Elsevier B.V., All rights reserved.",

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AU - Gustafsson, Jan Åke

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Development of subtype-selective oestrogen receptor-based therapeutics

Abstract

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