Top ▲

kynurenine 3-monooxygenase

Click here for help

Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2886

Nomenclature: kynurenine 3-monooxygenase

Family: Kynurenine 3-monooxygenase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 486 1q43 KMO kynurenine 3-monooxygenase 1
Mouse 2 479 1 H3 Kmo kynurenine 3-monooxygenase
Rat 2 478 13q25 Kmo kynurenine 3-monooxygenase
Previous and Unofficial Names Click here for help
kynurenine 3-hydroxylase | kynurenine 3-monooxygenase (kynurenine 3-hydroxylase)
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction Click here for help
EC Number:
Description Reaction Reference
L-kynurenine + NADPH + O2 <=> 3-hydroxy-L-kynurenine + NADP(+) + H2O

Download all structure-activity data for this target as a CSV file go icon to follow link

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK065 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 10.3 pKi 2
pKi 10.3 (Ki 5x10-11 M) [2]
GSK065 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.6 pIC50 2
pIC50 8.6 (IC50 2.5x10-9 M) [2]
GSK180 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.2 pIC50 3
pIC50 8.2 [3]
Description: Biochemical assay using human KMO expressed as a GST-fusion protein in a baculovirus expression system.
Immunopharmacology Comments
GSK180-induced inhibition of KMO prevents multiple organ failure in rodent models of acute pancreatitis which is caused by excessive alcohol consumption [3], and which is an inflammatory condition in humans for which there is no current therapy. A Phase 1 trial of GSK's clinical stage KMO inhibitor GSK065/GSK3335065 in healthy subjects was terminated (see NCT03245619).
Immuno Process Associations
Immuno Process:  Cytokine production & signalling


Show »

1. Alberati-Giani D, Cesura AM, Broger C, Warren WD, Röver S, Malherbe P. (1997) Cloning and functional expression of human kynurenine 3-monooxygenase. FEBS Lett, 410 (2-3): 407-12. [PMID:9237672]

2. Hutchinson JP, Rowland P, Taylor MRD, Christodoulou EM, Haslam C, Hobbs CI, Holmes DS, Homes P, Liddle J, Mole DJ et al.. (2017) Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase. Nat Commun, 8: 15827. [PMID:28604669]

3. Mole DJ, Webster SP, Uings I, Zheng X, Binnie M, Wilson K, Hutchinson JP, Mirguet O, Walker A, Beaufils B et al.. (2016) Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis. Nat Med, 22 (2): 202-9. [PMID:26752518]

How to cite this page Kynurenine 3-monooxygenase: kynurenine 3-monooxygenase. Last modified on 08/04/2019. Accessed on 24/07/2024. IUPHAR/BPS Guide to PHARMACOLOGY,