4.5 Review

Orphan Nuclear Receptors as Targets for Drug Development

Journal

PHARMACEUTICAL RESEARCH
Volume 27, Issue 8, Pages 1439-1468

Publisher

SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-010-0117-7

Keywords

agonist; antagonist; ligand binding domain; orphan nuclear receptor

Funding

  1. Damon Runyon Clinical Investigator Award [CI015-02]
  2. NCI [1R01CA127231-01]
  3. Albert Einstein College of Medicine, Bronx, NY

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Orphan nuclear receptors regulate diverse biological processes. These important molecules are ligand-activated transcription factors that act as natural sensors for a wide range of steroid hormones and xenobiotic ligands. Because of their importance in regulating various novel signaling pathways, recent research has focused on identifying xenobiotics targeting these receptors for the treatment of multiple human diseases. In this review, we will highlight these receptors in several physiologic and pathophysiologic actions and demonstrate how their functions can be exploited for the successful development of newer drugs.

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