hydroxysteroid 11-beta dehydrogenase 1 | 1.-.-.- Oxidoreductases | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

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hydroxysteroid 11-beta dehydrogenase 1

Target id: 2763

Nomenclature: hydroxysteroid 11-beta dehydrogenase 1

Abbreviated Name: 11-βHSD1

Family: 1.-.-.- Oxidoreductases

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 292 1q32-q41 HSD11B1 hydroxysteroid 11-beta dehydrogenase 1
Mouse - 292 1 97.67 cM Hsd11b1 hydroxysteroid 11-beta dehydrogenase 1
Rat - 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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human 11-beta-hydroxysteroid-dehydrogenase Bound to an Ortho-chlro-sulfonyl-piperazine Inhibitor
PDB Id:  3H6K
Ligand:  KB-74935
Resolution:  2.19Å
Species:  Human
References:  5
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ABT-384 Hs Inhibition 8.1 pKi 4
pKi 8.1 (Ki 9x10-9 M) [4]
AZD4017 Hs Inhibition 8.7 pIC50 3
pIC50 8.7 (IC50 2x10-9 M) [3]
BMS-823778 Hs Inhibition 8.6 pIC50 2
pIC50 8.6 (IC50 2.3x10-9 M) [2]
AZD8329 Hs Inhibition 8.1 pIC50 1
pIC50 8.1 (IC50 9x10-9 M) [1]
Clinically-Relevant Mutations and Pathophysiology
Disease:  Cortisone reductase deficiency 2
Synonyms: Hyperandrogenism due to cortisone reductase deficiency [Orphanet: ORPHA168588]
OMIM: 614662
Orphanet: ORPHA168588
General Comments
HSD11B1 reduces cortisone to the active hormone cortisol.


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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. 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]

3. 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]

4. 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]

5. 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]

How to cite this page

1.-.-.- Oxidoreductases: hydroxysteroid 11-beta dehydrogenase 1. Last modified on 12/12/2018. Accessed on 29/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2763.