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An Analysis of the Steroid Binding Domain of Receptors and of Ligand Structure and Binding Affinity

  • Chapter
Book cover The Steroid/Thyroid Hormone Receptor Family and Gene Regulation

Part of the book series: Birkhäuser Congress Reports Life Sciences ((ALS))

Summary

The steroid binding domains of the human progestin, glucocorticoid, mineralocorticoid, androgen, and estrogen receptors have been analysed by hydrophobic cluster analysis which enables a cogent alignment of amino-acid sequences and facilitates prediction of secondary structure features. Several regions of high sequence identity have been identified some of which could participate in steroid binding. The similarities among the receptors and the strong analogies with the 3D-structure of human corticosteroid binding globulin are discussed.

Many properties of a steroid may intervene in its interaction with the steroid binding domain: conformation, ability to form hydrogen bonds, van der Waals interactions, charge distribution… These aspects of steroid structure are illustrated by a choice of known as well as novel ligands. The crystal structures of several of these ligands have been established and the specificity and kinetics of their binding to steroid receptors have been determined in a routine screening system.

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Authors and Affiliations

  1. Roussel-Uclaf, 35 bd des Invalides, 75007, Paris, France

    J. P. Reynaud, T. Ojasoo & G. Teutsch

  2. Laboratoire de Minéralogie-Cristallographie, Université Pierre et Marie Curie, 4 Place Jussieu, 75252, Paris Cedex 05, France

    V. Bissery, C. Gaboriaud & J. P. Mornon

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  1. Dept. of Medical Nutrition, Karolinska Institute, Huddinge University Hospital F69, S-14186, Huddinge, Sweden

    Jan Carlstedt-Duke  & Jan-Åke Gustafsson  & 

  2. Reproductive Endocrinology, Research Unit, Karolinska Hospital, S-10401, Stockholm, Sweden

    Håkan Eriksson

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Reynaud, J.P., Bissery, V., Gaboriaud, C., Ojasoo, T., Teutsch, G., Mornon, J.P. (1989). An Analysis of the Steroid Binding Domain of Receptors and of Ligand Structure and Binding Affinity. In: Carlstedt-Duke, J., Eriksson, H., Gustafsson, JÅ. (eds) The Steroid/Thyroid Hormone Receptor Family and Gene Regulation. Birkhäuser Congress Reports Life Sciences. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-5466-5_24

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