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The importance of being varied in steroid receptor transactivation


The importance of being varied in steroid receptor transactivation



Trends in Pharmacological Sciences 24(5): 253-259



ISSN/ISBN: 0165-6147

PMID: 12767725

DOI: 10.1016/s0165-6147(03)00101-9

A major response of steroid receptors to steroid hormones is the induction of gene transcription. Two relevant, albeit less studied, properties of these receptors are the EC(50) values of the receptor-agonist complexes and the partial agonist activity of the receptor-antagonist complexes. Contrary to earlier expectations, neither the EC(50) value nor the partial agonist activity is constant for a given receptor-steroid complex. This variation is, however, beneficial to cells and organisms because it provides a mechanism both for differential control of gene expression by a single concentration of circulating hormone and for limiting side-effects during endocrine therapies. In this article, the factors and proposed mechanisms for the modulation of the EC(50) value and partial agonist activity of receptor-steroid complexes are discussed.

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Accession: 011515510

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