hydroxysteroid 11-beta dehydrogenase 1

Target id: 2763

Nomenclature: hydroxysteroid 11-beta dehydrogenase 1

Abbreviated Name: 11-βHSD1

Family: 1.-.-.- Oxidoreductases

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for hydroxysteroid 11-beta dehydrogenase 1 in GtoImmuPdb

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
corticosteroid 11-beta-dehydrogenase isozyme 1 | HSD11B | hydroxysteroid (11-beta) dehydrogenase 1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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:  4
Enzyme Reaction
EC Number: 1.1.1.146

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
ABT-384 Hs Inhibition 8.1 pKi 3
pKi 8.1 (Ki 9x10-9 M) [3]
AZD4017 Hs Inhibition 8.7 pIC50 2
pIC50 8.7 (IC50 2x10-9 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

References

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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. 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]

3. 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]

4. 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 13/08/2015. Accessed on 17/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2763.