Principles for modulation of the nuclear receptor superfamily

Hinrich Gronemeyer, Jan Åke Gustafsson, Vincent Laudet

Research output: Contribution to journalReview articlepeer-review

968 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)950-964
Number of pages15
JournalNature Reviews Drug Discovery
Issue number11
StatePublished - Nov 2004

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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