The importance of being varied in steroid receptor transactivation

Trends in Pharmacological Sciences
S Stoney Simons

Abstract

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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Citations

Mar 31, 2010·Proceedings of the National Academy of Sciences of the United States of America·Karen M OngCarson C Chow
Apr 26, 2014·Cell Research·Yuanzheng HeH Eric Xu
Jun 28, 2008·Molecular and Cellular Endocrinology·Yunguang SunS Stoney Simons
Jul 16, 2008·BioEssays : News and Reviews in Molecular, Cellular and Developmental Biology·S Stoney Simons
May 26, 2006·The Journal of Steroid Biochemistry and Molecular Biology·Yuli KimS Stoney Simons
Jun 15, 2011·Molecular and Cellular Endocrinology·S Stoney Simons, Carson C Chow
Jun 26, 2013·Molecular and Cellular Endocrinology·S Stoney Simons, Raj Kumar
Apr 19, 2006·Pediatric Allergy and Immunology : Official Publication of the European Society of Pediatric Allergy and Immunology·Michael KendlerEckehardt Jecht
Dec 16, 2015·Applied Developmental Science·Peter C ScalesTravis J Pashak
Mar 30, 2018·Frontiers in Endocrinology·Carson C Chow, S Stoney Simons
Aug 30, 2005·Molecular and Cellular Endocrinology·Dominique KoubovecJanet Patricia Hapgood

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