Steroid hormone receptors

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Steroid hormone receptors (nomenclature as agreed by NC-IUPHAR Committee on Nuclear Receptors, [1,3]) are nuclear hormone receptors of the NR3 class, with endogenous agonists that may be divided into 3-hydroxysteroids (estrone and E2) and 3-ketosteroids (DHT [DHT], aldosterone, cortisol, corticosterone, progesterone and testosterone). These receptors exist as dimers coupled with chaperone molecules (such as hsp90β (HSP90AB1, P08238) and immunophilin FKBP52:FKBP4, Q02790), which are shed on binding the steroid hormone. Although rapid signalling phenomena are observed [2,5], the principal signalling cascade appears to involve binding of the activated receptors to nuclear hormone response elements of the genome, with a 15-nucleotide consensus sequence AGAACAnnnTGTTCT (i.e. an inverted palindrome) as homo- or heterodimers. They also affect transcription by protein–protein interactions with other transcription factors, such as activator protein 1 (AP-1) and nuclear factor κB (NF-κB). Splice variants of each of these receptors can form functional or non-functional monomers that can dimerize to form functional or non-functional receptors. For example, alternative splicing of PR mRNA produces A and B monomers that combine to produce functional AA, AB and BB receptors with distinct characteristics [7].

A 7TM receptor responsive to estrogen (GPER1, Q99527, also known as GPR30, see [4]) has been described. Human orthologues of 7TM ‘membrane progestin receptors’ (PAQR7, PAQR8 and PAQR5), initially discovered in fish [8-9], appear to localize to intracellular membranes and respond to ‘non-genomic’ progesterone analogues independently of G proteins [6].

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How to cite this family page

Database page citation:

Steroid hormone receptors. Accessed on 29/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=107.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: Nuclear Hormone Receptors. Br J Pharmacol. 170: 1652–1675.