An Introduction to Nuclear Hormone Receptors
Nuclear hormone receptors are specialised transcription factors with commonalities of sequence and structure, which bind as homo- or heterodimers to specific consensus sequences of DNA (response elements) in the promoter region of particular target genes. They regulate (either promoting or repressing) transcription of these target genes in response to a variety of endogenous ligands. Endogenous agonists are hydrophobic entities which, when bound to the receptor promote conformational changes in the receptor to allow recruitment (or dissociation) of protein partners, generating a large multiprotein complex.
Two major subclasses of nuclear hormone receptors with identified endogenous agonists can be identified: steroid and non-steroid hormone receptors. Steroid hormone receptors function typically as dimeric entities and are thought to be resident outside the nucleus in the unliganded state in a complex with chaperone proteins, which are liberated upon agonist binding. Migration to the nucleus and interaction with other regulators of gene transcription, including RNA polymerase, acetyltransferases and deacetylases, allows gene transcription to be regulated. Non-steroid hormone receptors typically exhibit a greater distribution in the nucleus in the unliganded state and interact with other nuclear hormone receptors to form heterodimers, as well as with other regulators of gene transcription, leading to changes in gene transcription upon agonist binding.
Selectivity of gene regulation is brought about through interaction of nuclear hormone receptors with particular consensus sequences of DNA, which are arranged typically as repeats or inverted palindromes to allow accumulation of multiple transcription factors in the promoter regions of genes.
We wish to acknowledge the tremendous help provided by the Consultants to the Guides past and present (see list in the Overview, p. 1452). We are also extremely grateful for the financial contributions from the British Pharmacological Society, the International Union of Basic and Clinical Pharmacology, the Wellcome Trust (099156/Z/12/Z]), which support the website and the University of Edinburgh, who host the guidetopharmacology.org website.
Conflict of interest
The authors state that there is no conflict of interest to disclose.
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List of records presented
- 1654 1A. Thyroid Hormone Receptors
- 1655 1B. Retinoic acid receptors
- 1656 1C. Peroxisome proliferator-activated receptors
- 1657 1D. Rev-Erb receptors
- 1658 1F. Retinoic acid-related orphans
- 1659 1H. Liver X receptor-like receptors
- 1660 1I. Vitamin D receptor-like receptors
- 1661 2A. Hepatocyte nuclear factor-4 receptors
- 1662 2B. Retinoid X receptors
- 1663 2C. Testicular receptors
- 1664 2E. Tailless-like receptors
- 1665 2F. COUP-TF-like receptors
- 1666 3B. Estrogen-related receptors
- 1667 4A. Nerve growth factor IB-like receptors
- 1668 5A. Fushi tarazu F1-like receptors
- 1669 6A. Germ cell nuclear factor receptors
- 1670 0B. DAX-like receptors
- 1671 Steroid hormone receptors