TY - JOUR
T1 - Principles for modulation of the nuclear receptor superfamily
AU - Gronemeyer, Hinrich
AU - Gustafsson, Jan Åke
AU - Laudet, Vincent
N1 - Funding Information:
V.L. thanks S. Watson, J. Samarut and M. Schubert for critical reading of the manuscript as well as H. Escriva and J. Katzenellenbogen for help in preparation. H.G. would like to thank the members of his and D. Moras’ lab for discussions and figures. J.-Å.G. also thanks K. Koehler for discussions and for figures. Work in our laboratories is supported by grants from the Association for International Cancer Research, the Association pour la Recherche contre le Cancer, the Fondation de France, the European Community, Bristol-Myers Squibb, The Swedish Cancer Fund, The Swedish Science Council, KaroBio AB, Centre National de la Recherche Scientifique, Ministère de la Recherche et de la Technologie, and Région Rhône-Alpes. This publication is supported by the CASCADE network of excellence of the European Community.
PY - 2004/11
Y1 - 2004/11
N2 - 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.
AB - 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.
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U2 - 10.1038/nrd1551
DO - 10.1038/nrd1551
M3 - Review article
C2 - 15520817
AN - SCOPUS:8844262660
SN - 1474-1776
VL - 3
SP - 950
EP - 964
JO - Nature Reviews Drug Discovery
JF - Nature Reviews Drug Discovery
IS - 11
ER -