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Retinoids pp 215-235 | Cite as

RXR-Specific Agonists and Modulators: A New Retinoid Pharmacology

  • I. G. Schulman
  • D. Crombie
  • R. P. Bissonnette
  • R. Cesario
  • K. Roegner
  • G. Shao
  • R. A. Heyman
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 139)

Abstract

Receptors for retinoic acid (RARs and RXRs), thyroid hormone (TRs), vitamin D (VDR), prostanoids (PPARs) and numerous orphan receptors for which ligands have not been identified play vital roles in vertebrate cell growth, development, differentiation, metabolism and homcostasis. These receptors, like most members of the nuclear hormone receptor superfamily, function as hormone-dependent transcription factors that regulate the expression of large gene networks. The important biological activities of nuclear hormone receptors combined with the ability to directly regulate their activity with small molecules has long made this superfamily of transcription factors a target for drug discovery. This review focuses on the retinoid X receptors (RXRs), first characterized as receptors for the vitamin A derivative 9-cis retinoic acid (for recent reviews see Mangelsdorf and Evans 1995; Mangelsdorf et al. 1995; Perlmann and Evans 1997). Recent work demonstrating that ligands for RXR may provide effective treatments for several types of cancers as well as for type II diabetes has lead to great interest in this class of nuclear hormone receptors that until recently were thought of as a “silent partner.”

Keywords

Retinoic Acid Nuclear Hormone Receptor CREB Binding Protein 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer-Verlag Berlin Heidelberg 1999

Authors and Affiliations

  • I. G. Schulman
  • D. Crombie
  • R. P. Bissonnette
  • R. Cesario
  • K. Roegner
  • G. Shao
  • R. A. Heyman

There are no affiliations available

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