The corticosteroid receptors are receptors for corticosteroids.[1] Corticosteroid receptors mediate the target organ response to the major products of the adrenal cortex, glucocorticoids (principally cortisol in man), and mineralocorticoids (principally aldosterone). They are members of the intracellular receptor superfamily which is highly evolutionarily conserved, and includes receptors for thyroid hormones, vitamin D, sex steroids, and retinoids.[2] They include the following two nuclear receptors:[1][3][4]
There are also membrane corticosteroid receptors, including the membrane glucocorticoid receptors and the membrane mineralocorticoid receptors, which are not well-characterized at present.[5][6][7]
References
- ^ a b Scott T. Brady; George J. Siegel; Robert Wayne Albers; Donald Lowell Price (2012). Basic Neurochemistry: Principles of Molecular, Cellular and Medical Neurobiology. Academic Press. pp. 522–. ISBN 978-0-12-374947-5.
- ^ Walker, Brian R.; Stewart, Paul M.; Edwards, Christopher R.W. (1997), "Enzyme Modulation of Access to Corticosteroid Receptors", Molecular and Cellular Endocrinology, Principles of Medical Biology, vol. 10, Elsevier, pp. 297–310, doi:10.1016/s1569-2582(97)80038-4, ISBN 978-1-55938-815-3, retrieved 2024-07-15
- ^ Eugenia Wang; D. Stephen Snyder (13 August 1998). Handbook of the Aging Brain. Academic Press. pp. 22–. ISBN 978-0-08-053322-3.
- ^ Hormones, Brain and Behavior, Five-Volume Set. Academic Press. 18 June 2002. pp. 267–. ISBN 978-0-08-053415-2.
- ^ Groeneweg FL, Karst H, de Kloet ER, Joëls M (2012). "Mineralocorticoid and glucocorticoid receptors at the neuronal membrane, regulators of nongenomic corticosteroid signalling". Mol. Cell. Endocrinol. 350 (2): 299–309. doi:10.1016/j.mce.2011.06.020. PMID 21736918. S2CID 23048944.
- ^ Tasker JG, Di S, Malcher-Lopes R (2006). "Minireview: rapid glucocorticoid signaling via membrane-associated receptors". Endocrinology. 147 (12): 5549–56. doi:10.1210/en.2006-0981. PMC 3280589. PMID 16946006.
- ^ Dooley R, Harvey BJ, Thomas W (2012). "Non-genomic actions of aldosterone: from receptors and signals to membrane targets". Mol. Cell. Endocrinol. 350 (2): 223–34. doi:10.1016/j.mce.2011.07.019. PMID 21801805. S2CID 24630510.
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(1) Basic domains |
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(1.1) Basic leucine zipper (bZIP) | |
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(1.2) Basic helix-loop-helix (bHLH) | Group A | |
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Group B | |
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Group C bHLH-PAS | |
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Group D | |
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Group E | |
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Group F bHLH-COE | |
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(1.3) bHLH-ZIP | |
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(1.4) NF-1 | |
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(1.5) RF-X | |
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(1.6) Basic helix-span-helix (bHSH) | |
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(2) Zinc finger DNA-binding domains |
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(2.1) Nuclear receptor (Cys4) | subfamily 1 | |
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subfamily 2 | |
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subfamily 3 | |
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subfamily 4 | |
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subfamily 5 | |
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subfamily 6 | |
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subfamily 0 | |
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(2.2) Other Cys4 | |
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(2.3) Cys2His2 | |
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(2.4) Cys6 | |
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(2.5) Alternating composition | |
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(2.6) WRKY | |
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(4) β-Scaffold factors with minor groove contacts |
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(0) Other transcription factors |
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see also transcription factor/coregulator deficiencies |
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GRTooltip Glucocorticoid receptor | Agonists |
- Cortisol-like and related (16-unsubstituted): 3α,5α-Tetrahydrocorticosterone
- 5α-Dihydrocorticosterone
- 9α-Fluorocortisone (alfluorone)
- 11-Dehydrocorticosterone (11-oxocorticosterone, 17-deoxycortisone)
- 11-Dehydrocorticosterone acetate
- 11-Deoxycorticosterone (desoxycortone, deoxycortone, desoxycorticosterone)
- 11-Deoxycortisol (cortodoxone, cortexolone)
- Cortifen (cortiphen, kortifen)
- Cortodoxone acetate
- 21-Deoxycortisol
- Δ7-Prednisolone
- Δ7-Prednisolone 21-acetate
- Amebucort
- Chloroprednisone
- Cloprednol
- Corticosterone
- Corticosterone acetate
- Corticosterone benzoate
- Cortisol (hydrocortisone)
- Benzodrocortisone (hydrocortisone benzoate)
- Hydrocortamate (hydrocortisone diethylaminoacetate)
- Hydrocortisone esters
- Cortisone
- Deprodone
- Dichlorisone
- Dichlorisone acetate
- Dichlorisone diacetate
- Difluprednate
- Endrisone (endrysone)
- Etiprednol
- Etiprednol dicloacetate (etiprednol dichloroacetate)
- Fludrocortisone (fludrocortone)
- Fluorometholone
- Fluperolone
- Fluprednisolone
- Halopredone
- Halopredone acetate (halopredone diacetate)
- Isoflupredone (9α-fluoroprednisolone)
- Loteprednol
- Mazipredone (depersolone)
- Medrysone
- Methylprednisolone
- Methylprednisolone esters
- Prebediolone
- Prednisolone
- Prednazate
- Prednazoline
- Prednicarbate (prednisolone ethylcarbonate propionate)
- Prednimustine
- Prednisolamate (prednisolone diethylaminoacetate)
- Prednisolone esters
- Prednisone
- Pregnenolone
- Pregnenolone acetate
- Pregnenolone succinate (pregnenolone hemisuccinate)
- Resocortol
- Tipredane
- Tixocortol
- Butixocort (tixocortol butyrate)
- Tixocortol pivalate
- Methasones and related (16-substituted): 16α-Methyl-11-oxoprednisolone
- Alclometasone
- Alclometasone dipropionate
- Amelometasone
- Beclometasone (beclomethasone)
- Betamethasone (betametasone)
- Betamethasone esters
- Cortobenzolone (betamethasone salicylate)
- Ciclometasone (ciclomethasone, cyclomethasone)
- Clobetasol
- Clobetasone
- Clocortolone
- Cloticasone
- Cormetasone (cormethasone)
- Descinolone
- Desoximetasone (desoxymethasone)
- Dexamethasone (dexametasone)
- Diflorasone
- Diflucortolone
- Diflucortolone pivalate
- Diflucortolone valerate
- Dimesone
- Doxibetasol (doxybetasol)
- Fluclorolone
- Flumetasone (flumethasone)
- Flumetasone acetate
- Flumetasone pivalate
- Fluocinolone
- Fluocortin
- Fluocortin butyl (fluocortin butylate)
- Fluocortolone
- Fluprednidene (fluprednylidene)
- Fluticasone
- Fluticasone furoate
- Fluticasone propionate
- Halocortolone
- Halometasone
- Icometasone
- Icometasone enbutate (icometasone butyrate acetate)
- Isoprednidene
- Locicortolone (locicortone)
- Locicortolone dicibate (locicortone dicibate)
- Meclorisone
- Meprednisone (methylprednisone)
- Meprednisone acetate
- Meprednisone hydrogen succinate (methylprednisone hemisuccinate)
- Mometasone
- Paramethasone
- Paramethasone acetate
- Paramethasone disodium phosphate
- Paramethasone phosphate
- Prednylidene
- Prednylidene diethylaminoacetate
- Rimexolone
- Ticabesone
- Timobesone
- Triamcinolone
- Ulobetasol (halobetasol)
- Vamorolone
- Cyclic ketals (16,17-cyclized): Acrocinonide (triamcinolone acroleinide)
- Amcinafal (triamcinolone pentanonide)
- Amcinafide (triamcinolone acetophenide)
- Amcinonide (triamcinolone acetate cyclopentanonide)
- Budesonide
- Ciclesonide
- Cicortonide
- Deflazacort (azacort)
- Descinolone acetonide
- Desonide (hydroxyprednisolone acetonide)
- Desonide disodium phosphate
- Desonide pivalate
- Dexbudesonide
- Drocinonide
- Fluazacort
- Fluclorolone acetonide (flucloronide)
- Fludroxycortide (flurandrenolone, flurandrenolide)
- Flumoxonide
- Flunisolide
- Fluocinolone acetonide
- Ciprocinonide (fluocinolone acetonide cyclopropylcarboxylate)
- Fluocinonide (fluocinolide, fluocinolone acetonide acetate)
- Procinonide (fluocinolone acetonide propionate)
- Formocortal
- Halcinonide
- Itrocinonide
- Rofleponide
- Tralonide
- Triamcinolone acetonide
- Flupamesone (triamcinolone acetonide metembonate)
- Triamcinolone acetonide esters
- Triamcinolone aminobenzal benzamidoisobutyrate (TBI-PAB)
- Triclonide
- Others/atypical (other expanded steroid ring systems, homosteroids, and non-pregnane steroids): Cortisuzol
- Cortivazol
- Domoprednate
- Naflocort
- Nicocortonide
- Nivacortol (nivazol)
- Oxisopred
- RU-26988
- RU-28362
- Non-corticosteroids with some glucocorticoid activity: 15β-Hydroxycyproterone acetate
- 17α-Hydroxyprogesterone
- Bromoketoprogesterone
- Chlormadinone acetate
- Cyproterone
- Cyproterone acetate
- Danazol
- Delmadinone acetate
- Desogestrel
- DU-41165
- Etonogestrel
- Flugestone
- Flugestone acetate (flurogestone acetate)
- Fluoromedroxyprogesterone acetate
- Fluoxymesterone
- Gestodene
- Medrogestone
- Medroxyprogesterone acetate
- Megestrol acetate
- Metribolone
- Norgestomet
- Osaterone acetate
- Progesterone
- Promegestone
- RU-2309
- Quingestrone
- Segesterone acetate (nestorone)
- Tetrahydrogestrinone
- Nonsteroidal glucocorticoids: AZD-5423
- GSK-9027
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Mixed (SEGRMsTooltip Selective glucocorticoid receptor agonists) |
- Dagrocorat
- Fosdagrocorat
- Mapracorat
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Antagonists |
- 7α-Hydroxy-DHEA
- 17α-Methylprogesterone
- Aglepristone
- Asoprisnil
- Asoprisnil ecamate
- C108297
- C113176
- CORT-108297
- Cyproterone acetate
- Dazucorilant
- Exicorilant (CORT-125281)
- Guggulsterone
- Ketoconazole
- Lilopristone
- LLY-2707
- Metapristone (RU-42633)
- Miconazole
- Mifepristone (RU-486)
- Miricorilant (CORT-118335)
- Onapristone
- ORG-34116
- ORG-34517 (SCH-900636)
- ORG-34850
- Pregnenolone 16α-carbonitrile
- Relacorilant (CORT-125134)
- RTI 3021–012
- RTI 3021–022
- Telapristone
- Tibolone
- Toripristone
- Ulipristal acetate
- Zavacorilant
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Others |
- Antisense oligonucleotides: IONIS-GCCRRx (ISIS-426115)
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- See also
- Receptor/signaling modulators
- Glucocorticoids and antiglucocorticoids
- Mineralocorticoid receptor modulators
- List of corticosteroids
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MRTooltip Mineralocorticoid receptor | Agonists | |
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Antagonists |
- Steroidal: 6β-Hydroxy-7α-thiomethylspironolactone
- 7α-Acetylthio-17α-hydroxyprogesterone
- 7α-Thiomethylspironolactone (SC-26519)
- 7α-Thioprogesterone (SC-8365)
- 7α-Thiospironolactone (SC-24813)
- 16α-Hydroxyprogesterone
- 17α-Hydroxyprogesterone (hydroxyprogesterone)
- 18-Deoxyaldosterone
- 18,19-Dinorprogesterone
- Canrenoate potassium (potassium canrenoate)
- Canrenoic acid (canrenoate)
- Canrenone (canrenoate y-lactone)
- Dicirenone
- Dimethisterone
- Drospirenone
- Dydrogesterone
- Eplerenone
- Gestodene
- Guggulsterone
- Hydroxyprogesterone caproate
- Medrogestone
- Mespirenone
- Metribolone
- Mexrenoate potassium
- Mexrenoic acid (mexrenoate)
- Mexrenone
- Oxprenoic acid (oxprenoate)
- Oxprenoate potassium (RU-28318)
- Pregnenolone
- Progesterone
- Prorenoate potassium
- Prorenoic acid (prorenoate)
- Prorenone
- RO-14-9012
- RU-26752
- SC-5233 (spirolactone)
- SC-8109
- SC-11927 (CS-1)
- SC-19886
- SC-27169
- Spirorenone
- Spironolactone
- Spiroxasone
- Tibolone
- Trimegestone
- Vamorolone
- ZK-91587
- ZK-97894
- Nonsteroidal: Amlodipine
- Apararenone
- Benidipine
- BR-4628
- Esaxerenone
- Felodipine
- Finerenone
- Miricorilant (CORT-118335)
- Nifedipine
- Nimodipine
- Nitrendipine
- Ocedurenone
- PF-03882845
- SM-368229
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- See also
- Receptor/signaling modulators
- Mineralocorticoids and antimineralocorticoids
- Glucocorticoid receptor modulators
- List of corticosteroids
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