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Target not currently curated in GtoImmuPdb
Target id: 2763
Nomenclature: hydroxysteroid 11-beta dehydrogenase 1
Abbreviated Name: 11-βHSD1
Family: 1.-.-.- Oxidoreductases
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 1 | 292 | 1q32.2 | HSD11B1 | hydroxysteroid 11-beta dehydrogenase 1 | |
Mouse | 1 | 292 | 1 H6 | Hsd11b1 | hydroxysteroid 11-beta dehydrogenase 1 | |
Rat | 1 | 288 | 13q27 | Hsd11b1 | hydroxysteroid 11-beta dehydrogenase 1 |
Previous and Unofficial Names ![]() |
11β-HSD | 11b-HSD | corticosteroid 11-beta-dehydrogenase isozyme 1 | HSD11B | hydroxysteroid (11-beta) dehydrogenase 1 |
Database Links ![]() |
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BRENDA | 1.1.1.146 |
ChEMBL Target | CHEMBL4235 (Hs), CHEMBL3910 (Mm), CHEMBL2391 (Rn) |
Ensembl Gene | ENSG00000117594 (Hs), ENSMUSG00000016194 (Mm), ENSRNOG00000005861 (Rn) |
Entrez Gene | 3290 (Hs), 15483 (Mm), 25116 (Rn) |
Human Protein Atlas | ENSG00000117594 (Hs) |
KEGG Enzyme | 1.1.1.146 |
KEGG Gene | hsa:3290 (Hs), mmu:15483 (Mm), rno:25116 (Rn) |
Pharos | P28845 (Hs) |
RefSeq Nucleotide | NM_181755 (Hs), NM_005525 (Hs), NM_001206741 (Hs), NM_001044751 (Mm), NM_008288 (Mm), NM_017080 (Rn) |
RefSeq Protein | NP_005516 (Hs), NP_001193670 (Hs), NP_861420 (Hs), NP_001038216 (Mm), NP_032314 (Mm), NP_058776 (Rn) |
UniProtKB | P28845 (Hs), P50172 (Mm), P16232 (Rn) |
Wikipedia | HSD11B1 (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific inhibitor tables |
Clinically-Relevant Mutations and Pathophysiology ![]() |
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General Comments |
HSD11B1 reduces cortisone to the active hormone cortisol. |
1. AstraZeneca. AZD8329. Accessed on 12/09/2014. Modified on 12/09/2014. astrazeneca.com, http://openinnovation.astrazeneca.com/what-we-offer/compound/azd8329/
2. Beseda I, Czollner L, Shah PS, Khunt R, Gaware R, Kosma P, Stanetty C, Del Ruiz-Ruiz MC, Amer H, Mereiter K et al.. (2010) Synthesis of glycyrrhetinic acid derivatives for the treatment of metabolic diseases. Bioorg Med Chem, 18 (1): 433-54. [PMID:19914836]
3. Chen XQ, Shao LD, Pal M, Shen Y, Cheng X, Xu G, Peng LY, Wang K, Pan ZH, Li MM et al.. (2015) Hupehenols A-E, selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors from Viburnum hupehense. J Nat Prod, 78 (2): 330-4. [PMID:25590374]
4. Li J, Kennedy LJ, Walker SJ, Wang H, Li JJ, Hong Z, O'Connor SP, Ye XY, Chen S, Wu S et al.. (2018) Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1). ACS Med Chem Lett, 9 (12): 1170-1174. DOI: 10.1021/acsmedchemlett.8b00307 [PMID:30613321]
5. Scott JS, Bowker SS, Deschoolmeester J, Gerhardt S, Hargreaves D, Kilgour E, Lloyd A, Mayers RM, McCoull W, Newcombe NJ et al.. (2012) Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017). J Med Chem, 55 (12): 5951-64. [PMID:22691057]
6. Sorensen B, Rohde J, Wang J, Fung S, Monzon K, Chiou W, Pan L, Deng X, Stolarik D, Frevert EU et al.. (2006) Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction. Bioorg Med Chem Lett, 16 (23): 5958-62. [PMID:16996734]
7. Wan ZK, Chenail E, Xiang J, Li HQ, Ipek M, Bard J, Svenson K, Mansour TS, Xu X, Tian X et al.. (2009) Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model. J Med Chem, 52 (17): 5449-61. [PMID:19673466]
8. Yang H, Shen Y, Chen J, Jiang Q, Leng Y, Shen J. (2009) Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors. Eur J Med Chem, 44 (3): 1167-71. [PMID:18653260]
1.-.-.- Oxidoreductases: hydroxysteroid 11-beta dehydrogenase 1. Last modified on 01/10/2020. Accessed on 11/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2763.