3C. 3-Ketosteroid receptors in GtoPdb v.2023.1

Apr 2023

Steroid hormone receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [75, 218, 3]) are nuclear hormone receptors of the NR3 class, with endogenous agonists that may be divided into 3-hydroxysteroids (estrone and 17β-estradiol) and 3-ketosteroids (dihydrotestosterone [DHT], aldosterone, cortisol, corticosterone, progesterone and testosterone). For rodent GR and MR, the physiological ligand is corticosterone rather than cortisol.

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3C. 3-Ketosteroid receptors in GtoPdb v.2023.1

IUPHAR/BPS Guide to Pharmacology CITE https://doi.org/10.2218/gtopdb/F98/2023.1 3C. 3-Ketosteroid receptors in GtoPdb v.2023.1 Derek Cain1, John Cidlowski1, Dean P. Edwards2, Peter Fuller3, Sandra L. Grimm2, Sean Hartig2, Carol A. Lange4, Robert H. Oakley1, Jennifer K. Richer5, Carol A. Sartorius5, Marc Tetel6, Nancy Weigel2 and Morag J. Young7 1. National Institutes of Health, USA 2. Baylor College of Medicine, USA 3. Hudson Instiitute of Medical Research, Australia 4. University of Minnesota, USA 5. University of Colorado, USA 6. Wellesley College, USA 7. Baker Heart and Diabetes Institute, Australia Abstract Steroid hormone receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [75, 218, 3]) are nuclear hormone receptors of the NR3 class, with endogenous agonists that may be divided into 3-hydroxysteroids (estrone and 17β-estradiol) and 3-ketosteroids (dihydrotestosterone [DHT], aldosterone, cortisol, corticosterone, progesterone and testosterone). For rodent GR and MR, the physiological ligand is corticosterone rather than cortisol. Contents This is a citation summary for 3C. 3-Ketosteroid receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links. GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts. For further details see [41]. Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators. Database links 3C. 3-Ketosteroid receptors https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=98 Introduction to 3C. 3-Ketosteroid receptors https://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=98 Receptors Androgen receptor https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=628 Glucocorticoid receptor https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=625 Mineralocorticoid receptor https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=626 Progesterone receptor https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=627 References 1. Ahrens-Fath I, Politz O, Geserick C and Haendler B. (2005) Androgen receptor function is modulated by the tissue-specific AR45 variant. FEBS J 272: 74-84 [PMID:15634333] 2. Akita K, Harada K, Ichihara J, Takata N, Takahashi Y and Saito K. (2013) A novel selective androgen receptor modulator, NEP28, is efficacious in muscle and brain without serious side effects on prostate. Eur J Pharmacol 720: 107-14 [PMID:24177288] 3. Alexander SPH, Cidlowski JA, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD and Pawson AJ et al.. (2019) THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Nuclear hormone receptors. Br J Pharmacol 176 Suppl 1: S229-S246 [PMID:31710718] 4. Amasheh S, Epple HJ, Mankertz J, Detjen K, Goltz M, Schulzke JD and Fromm M. (2000) Differential regulation of ENaC by aldosterone in rat early and late distal colon. Ann N Y Acad Sci 915: 92-4 [PMID:11193605] 5. Antonarakis ES, Lu C, Wang H, Luber B, Nakazawa M, Roeser JC, Chen Y, Mohammad TA, Chen Y and Fedor HL et al.. (2014) AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer. N Engl J Med 371: 1028-38 [PMID:25184630] 6. Anzick SL, Kononen J, Walker RL, Azorsa DO, Tanner MM, Guan XY, Sauter G, Kallioniemi OP, Trent JM and Meltzer PS. (1997) AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer. Science 277: 965-8 [PMID:9252329] 7. Arriza JL, Weinberger C, Cerelli G, Glaser TM, Handelin BL, Housman DE and Evans RM. (1987) Cloning of human mineralocorticoid receptor complementary DNA: structural and functional kinship with the glucocorticoid receptor. Science 237: 268-75 [PMID:3037703] 8. Attia GR, Zeitoun K, Edwards D, Johns A, Carr BR and Bulun SE. (2000) Progesterone receptor isoform A but not B is expressed in endometriosis. J Clin Endocrinol Metab 85: 2897-902 [PMID:10946900] 9. Auerbach SS. DrugMatrix in vitro pharmacology data https://ntp.niehs.nih.gov/drugmatrix/index.html. Accessed on 30/04/2019. 10. Auerbach SS and DrugMatrix® and ToxFX® Coordinator National Toxicology Program.. National Toxicology Program: Dept of Health and Human Services. https://ntp.niehs.nih.gov/drugmatrix/index.html. Accessed on 02/05/2014. 11. Aupperlee MD, Smith KT, Kariagina A and Haslam SZ. (2005) Progesterone receptor isoforms A and B: temporal and spatial differences in expression during murine mammary gland development. Endocrinology 146: 3577-88 [PMID:15878961] 12. Bamberger AM, Milde-Langosch K, Schulte HM and Löning T. (2000) Progesterone receptor isoforms, PR-B and PR-A, in breast cancer: correlations with clinicopathologic tumor parameters and expression of AP-1 factors. Horm Res 54: 32-7 [PMID:11182633] 13. Barik J, Marti F, Morel C, Fernandez SP, Lanteri C, Godeheu G, Tassin JP, Mombereau C, Faure P and Tronche F. (2013) Chronic stress triggers social aversion via glucocorticoid receptor in dopaminoceptive neurons. Science 339: 332-5 [PMID:23329050] 14. Barnes PJ, Greening AP and Crompton GK. (1995) Glucocorticoid resistance in asthma. Am J Respir Crit Care Med 152: S125-40 [PMID:7489120] 15. Beggah AT, Escoubet B, Puttini S, Cailmail S, Delage V, Ouvrard-Pascaud A, Bocchi B, Peuchmaur M, Delcayre C, Farman N and Jaisser F. (2002) Reversible cardiac fibrosis and heart failure induced by conditional expression of an antisense mRNA of the mineralocorticoid receptor in cardiomyocytes. Proc Natl Acad Sci USA 99: 7160-5 [PMID:11997477] 16. Bell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA and Richey R et al.. (2007) (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}- methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor. J Med Chem 50: 6443-5 [PMID:18038968] 17. Belvisi MG, Bundschuh DS, Stoeck M, Wicks S, Underwood S, Battram CH, Haddad el-B, Webber SE and Foster ML. (2005) Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma. J Pharmacol Exp Ther 314: 568-74 [PMID:15878996] 18. Bentvelsen FM, McPhaul MJ, Wil (...truncated)


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Derek Cain, John Cidlowski, Dean P. Edwards, Peter Fuller, Sandra L. Grimm, Sean Hartig, Carol A. Lange, Robert H. Oakley, Jennifer K. Richer, Carol A. Sartorius, Marc Tetel, Nancy Weigel, Morag J. Young. 3C. 3-Ketosteroid receptors in GtoPdb v.2023.1, 2023, Volume 2023, Issue 1,