The glucocorticoid receptor .
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 .
(1) Basic domains
(1.1) Basic leucine zipper (bZIP )(1.2) Basic helix-loop-helix (bHLH )
Group A Group B Group C bHLH-PAS Group D Group E Group F bHLH-COE
(1.3) bHLH-ZIP (1.4) NF-1 (1.5) RF-X (1.6) Basic helix-span-helix (bHSH)
(2) Zinc finger DNA-binding domains
(2.1) Nuclear receptor (Cys4 )
subfamily 1 subfamily 2 subfamily 3 subfamily 4 subfamily 5 subfamily 6 subfamily 0
(2.2) Other Cys4 (2.3) Cys2 His2 (2.4) Cys6 (2.5) Alternating composition (2.6) WRKY
(4) β-Scaffold factors with minor groove contacts
(0) Other transcription factors
see also transcription factor/coregulator deficiencies
GR Tooltip 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
Mixed (SEGRMs Tooltip Selective glucocorticoid receptor agonists )
Dagrocorat
Fosdagrocorat
Mapracorat
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
Others
Antisense oligonucleotides: IONIS-GCCRRx (ISIS-426115)
See also
Receptor/signaling modulators
Glucocorticoids and antiglucocorticoids
Mineralocorticoid receptor modulators
List of corticosteroids
MR Tooltip Mineralocorticoid receptor
Agonists 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
See also
Receptor/signaling modulators
Mineralocorticoids and antimineralocorticoids
Glucocorticoid receptor modulators
List of corticosteroids