Glucocorticoid

Glucocorticoid
Drug class
Chemical structure of cortisol (hydrocortisone), an endogenous glucocorticoid as well as a medication.
Class identifiers
SynonymsCorticosteroid; Glucocorticosteroid
UseAdrenal insufficiency; allergic, inflammatory, and autoimmune disorders; asthma; organ transplant
ATC codeH02AB
Biological targetGlucocorticoid receptor
Chemical classSteroids
Legal status
In Wikidata

Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor[1] that is present in almost every vertebrate animal cell. The name "glucocorticoid" is a portmanteau (glucose + cortex + steroid) and is composed from its role in regulation of glucose metabolism, synthesis in the adrenal cortex, and its steroidal structure (see structure below).

Glucocorticoids are part of the feedback mechanism in the immune system, which reduces certain aspects of immune function, such as inflammation. They are therefore used in medicine to treat diseases caused by an overactive immune system, such as allergies, asthma, autoimmune diseases, and sepsis. Glucocorticoids have many diverse effects such as pleiotropy, including potentially harmful side effects.[2] They also interfere with some of the abnormal mechanisms in cancer cells, so they are used in high doses to treat cancer. This includes inhibitory effects on lymphocyte proliferation, as in the treatment of lymphomas and leukemias, and the mitigation of side effects of anticancer drugs.

Glucocorticoids affect cells by binding to the glucocorticoid receptor. The activated glucocorticoid receptor-glucocorticoid complex up-regulates the expression of anti-inflammatory proteins in the nucleus (a process known as transactivation) and represses the expression of pro-inflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus (transrepression).[2]

Glucocorticoids are distinguished from mineralocorticoids and sex steroids by their specific receptors, target cells, and effects. In technical terms, "corticosteroid" refers to both glucocorticoids and mineralocorticoids (as both are mimics of hormones produced by the adrenal cortex), but is often used as a synonym for "glucocorticoid". Glucocorticoids are chiefly produced in the zona fasciculata of the adrenal cortex, whereas mineralocorticoids are synthesized in the zona glomerulosa.

Cortisol (or hydrocortisone) is the most important human glucocorticoid. It is essential for life, and it regulates or supports a variety of important cardiovascular, metabolic, immunologic, and homeostatic functions. Increases in glucocorticoid concentrations are an integral part of stress response and are the most commonly used biomarkers to measure stress.[3] Glucocorticoids have numerous non-stress-related functions as well, and glucocorticoid concentrations can increase in response to pleasure or excitement.[4] Various synthetic glucocorticoids are available; these are widely utilized in general medical practice and numerous specialties, either as replacement therapy in glucocorticoid deficiency or to suppress the body's immune system.

  1. ^ Pelt AC (2011). Glucocorticoids: effects, action mechanisms, and therapeutic uses. Hauppauge, N.Y.: Nova Science. ISBN 978-1617287589.[page needed]
  2. ^ a b Rhen T, Cidlowski JA (Oct 2005). "Antiinflammatory action of glucocorticoids–new mechanisms for old drugs". The New England Journal of Medicine. 353 (16): 1711–1723. doi:10.1056/NEJMra050541. PMID 16236742. S2CID 5744727.
  3. ^ Botía M, Escribano D, Martínez-Subiela S, Tvarijonaviciute A, Tecles F, López-Arjona M, et al. (January 2023). "Different Types of Glucocorticoids to Evaluate Stress and Welfare in Animals and Humans: General Concepts and Examples of Combined Use". Metabolites. 13 (1): 106. doi:10.3390/metabo13010106. PMC 9865266. PMID 36677031.
  4. ^ Ralph CR, Tilbrook AJ (February 2016). "INVITED REVIEW: The usefulness of measuring glucocorticoids for assessing animal welfare". Journal of Animal Science. 94 (2): 457–470. doi:10.2527/jas.2015-9645. PMID 27065116.

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