Abstract
Nuclear receptors constitute a special class of transcription factors that are activated by an extracellular signal. This signal is a hydrophobic substance, such as a steroid hormone, which can cross the plasma membrane and does not require a surface receptor to recognise it and transmit to the nucleus the information it conveys. The intracellular receptor is in charge of this function and of the regulation of target gene expression, after having recognised and bound its ligands. This is the most obvious difference between steroid hormones and polypeptidic hormones, which are recognised by G-protein-coupled receptors (GPCRs) (Chap. 6).
Nuclear receptors are the targets of many drugs aimed at treating metabolic and endocrinal diseases, drugs that can be agonists or antagonists of receptor activity. Two types of frequent cancers are hormone dependent: breast and prostate cancers. The nuclear receptors of oestrogens and androgens are, therefore, of major importance in oncology, because their alterations can participate to oncogenesis and cancer development and because they constitute major therapeutic targets. The hormonal treatments of breast cancer were historically the first ‘targeted therapies’ of cancers, but other nuclear receptors also present a major interest in oncology.
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Robert, J. (2015). Nuclear Receptor Pathways. In: Textbook of Cell Signalling in Cancer. Springer, Cham. https://doi.org/10.1007/978-3-319-14340-8_14
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DOI: https://doi.org/10.1007/978-3-319-14340-8_14
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