insulin degrading enzyme

Target id: 2371

Nomenclature: insulin degrading enzyme

Family: M16: Pitrilysin

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for insulin degrading enzyme in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1019 10q23-q25 IDE insulin degrading enzyme
Mouse - 1019 19 C2 Ide insulin degrading enzyme
Rat - 1019 1q53 Ide insulin degrading enzyme
Previous and Unofficial Names
INSDEGM | insulin protease | insulinase | insulysin
Database Links
Specialist databases
MEROPS M16.982 (Hs)
Other databases
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of insulin degrading enzyme complexed with inhibitor NTE-1.
PDB Id:  4PF9
Ligand:  NTE-1
Resolution:  2.5Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of insulin degrading enzyme complexed with inhibitor quinoline 2.
PDB Id:  4PF7
Ligand:  quinoline 2
Resolution:  2.33Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of insulin degrading enzyme complexed with inhibitor NTE-2
PDB Id:  4PFC
Ligand:  NTE-2
Resolution:  2.21Å
Species:  Human
References:  1
Enzyme Reaction
EC Number: 3.4.24.56

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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
NTE-1 Hs Inhibition 8.4 pIC50 1
pIC50 8.4 (IC50 4x10-9 M) [1]
NTE-2 Hs Inhibition 7.7 pIC50 1
pIC50 7.7 (IC50 1.8x10-8 M) [1]
quinoline 2 Hs Inhibition 5.7 pIC50 1
pIC50 5.7 (IC50 2x10-6 M) [1]

References

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1. Durham TB, Toth JL, Klimkowski VJ, Cao JX, Siesky AM, Alexander-Chacko J, Wu GY, Dixon JT, McGee JE, Wang Y et al.. (2015) Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in vivo. J. Biol. Chem.,  [Epub ahead of print]. [PMID:26085101]

How to cite this page

M16: Pitrilysin: insulin degrading enzyme. Last modified on 30/03/2016. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2371.