Proteins > Corticosteroid 11-beta-dehydrogenase isozyme 1
Page last updated: 2024-08-07 18:33:20
Corticosteroid 11-beta-dehydrogenase isozyme 1
An 11-beta-hydroxysteroid dehydrogenase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P28845]
Synonyms
EC 1.1.1.146;
11-beta-hydroxysteroid dehydrogenase 1;
11-DH;
11-beta-HSD1;
Short chain dehydrogenase/reductase family 26C member 1
Research
Bioassay Publications (38)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (26.32) | 29.6817 |
| 2010's | 25 (65.79) | 24.3611 |
| 2020's | 3 (7.89) | 2.80 |
Compounds (21)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| glycyrrhizic acid | Homo sapiens (human) | EC50 | 0.0100 | 1 | 1 |
| pf 915275 | Homo sapiens (human) | EC50 | 0.0100 | 3 | 3 |
Synthesis of selective 11β-HSD1 inhibitors based on dammarane scaffold.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Limonoids and Triterpenoids as 11β-HSD1 Inhibitors from Walsura robusta.Journal of natural products, , Apr-22, Volume: 79, Issue:4, 2016
Hupehenols A-E, selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors from Viburnum hupehense.Journal of natural products, , Feb-27, Volume: 78, Issue:2, 2015
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11β-HSD1 inhibitors: potential impact in diabetes.European journal of medicinal chemistry, , Volume: 65, 2013
Potent and novel 11β-HSD1 inhibitors identified from shape and docking based virtual screening.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 19, Issue:6, 2011
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:3, 2009
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11β-hydroxysteroid dehydrogenases.Journal of natural products, , Apr-27, Volume: 75, Issue:4, 2012
Cyclopeptide Alkaloids from Ziziphus apetala.Journal of natural products, , Dec-27, Volume: 74, Issue:12, 2011
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 19, Issue:6, 2011
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 69, 2022
Optimization of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Mechanistic Insight on the Mode of Action of Colletoic Acid.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors.ACS medicinal chemistry letters, , Feb-09, Volume: 3, Issue:2, 2012
Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 69, 2022
Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11β-HSD1 inhibitors: potential impact in diabetes.European journal of medicinal chemistry, , Volume: 65, 2013
Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.ACS medicinal chemistry letters, , Oct-11, Volume: 3, Issue:10, 2012
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Mechanistic Insight on the Mode of Action of Colletoic Acid.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 23, Issue:8, 2013
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 2011
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| 7-beta-hydroxysteroid dehydrogenase (NADP+) activity | molecular function | Catalysis of the reaction: NADP+ + a 7-beta-hydroxysteroid = NADPH + H+ + a 7-oxosteroid. [EC:1.1.1.201, MetaCyc:1.1.1.201-RXN] |
| NADP binding | molecular function | Binding to nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions; binding may be to either the oxidized form, NADP+, or the reduced form, NADPH. [GOC:ai] |
| 11-beta-hydroxysteroid dehydrogenase (NADP+) activity | molecular function | Catalysis of the reaction: an 11-beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+. [RHEA:11388] |
| cortisol dehydrogenase activity | molecular function | Catalysis of the reaction: cortisol + NADP = cortisone + NADPH + H+. [GOC:pz, PMID:16216911, RHEA:68616] |
| steroid binding | molecular function | Binding to a steroid, any of a large group of substances that have in common a ring system based on 1,2-cyclopentanoperhydrophenanthrene. [GOC:jl, ISBN:0198506732] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
Involved In
This protein is involved in 2 target(s):
| Target | Category | Definition |
|---|
| lung development | biological process | The process whose specific outcome is the progression of the lung over time, from its formation to the mature structure. In all air-breathing vertebrates the lungs are developed from the ventral wall of the oesophagus as a pouch which divides into two sacs. In amphibians and many reptiles the lungs retain very nearly this primitive sac-like character, but in the higher forms the connection with the esophagus becomes elongated into the windpipe and the inner walls of the sacs become more and more divided, until, in the mammals, the air spaces become minutely divided into tubes ending in small air cells, in the walls of which the blood circulates in a fine network of capillaries. In mammals the lungs are more or less divided into lobes, and each lung occupies a separate cavity in the thorax. [GOC:jid, UBERON:0002048] |
| steroid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus. [GOC:go_curators] |