Abstract

Nuclear receptors are major targets for drug discovery and have key roles in development and homeostasis, as well as in many diseases such as obesity, diabetes and cancer. This review provides a general overview of the mechanism of action of nuclear receptors and explores the various factors that are instrumental in modulating their pharmacology. In most cases, the response of a given receptor to a particular ligand in a specific tissue will be dictated by the set of proteins with which the receptor is able to interact. One of the most promising aspects of nuclear receptor pharmacology is that it is now possible to develop ligands with a large spectrum of full, partial or inverse agonist or antagonist activities, but also compounds, called selective nuclear receptor modulators, that activate only a subset of the functions induced by the cognate ligand or that act in a cell-type-selective manner.

Author affiliations

1. Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC) CNRS/INSERM/ULP, 1 rue Laurent Fries, BP 10142, 67404 Illkirch Cedex, C.U. de Strasbourg, France.
2. Karolinska Institute, Department of Medical Nutrition and Center of Biotechnology, Novum, S-141 86 Huddinge, Sweden.
3. Laboratoire de Biologie Moléculaire de la Cellule, CNRS UMR 5161, INRA LA 1237, Ecole Normale Supérieure de Lyon, 46, Allée d'Italie, 69364 Lyon Cedex 07, France.

Correspondence to: Vincent Laudet³ Email: Vincent.Laudet@ens-lyon.fr

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