Brand  (β version)

PDB ID: 6BYZ

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Ligands
Code Name Style Show Link
J18 [(8r,9s,10s)-9-(2',3'-dimethyl[1,1'-biphenyl]-4-yl)-6-{[2-(trifluoromethyl)phenyl]sulfonyl}-1,6-diazabicyclo[6.2.0]decan-10-yl]methanol PoSSuM
EPE 4-(2-hydroxyethyl)-1-piperazine ethanesulfonic acid PoSSuM
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Structure summary

Code : 6BYZ   PDBj   RCSB PDB   PDBe
Header : HYDROLASE/INHIBITOR
Title : Structure of Cysteine-free Human Insulin-Degrading Enzyme in complex with Substrate-selective Macrocyclic Inhibitor 37
Release Data : 2019-04-03
Compound :
mol_id molecule chains synonym
1 Insulin-degrading enzyme A,B Abeta-degrading protease,Insulin protease,Insulinase,Insulysin
ec: 3.4.24.56
mutation: C110L, E111Q, C171S, C178A, C257V, C414L, C573N, C590S, C789S, C812A, C819A, C904S, C966N, C974A
mol_id molecule chains
2 ALA-ALA-ALA D,E
other_details: Polypeptide co-purified with Human Insulin-Degrading enzyme
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli BL21(DE3)  (taxid:469008)
gene: IDE
expression_system_strain: BL21(DE3)
mol_id organism_scientific
2 Escherichia coli BL21(DE3)  (taxid:469008)
Authors : Tan, G.A., Seeliger, M.A., Maianti, J.P., Liu, D.R.
Keywords : Insulin, Glucagon, Diabetes, Exo-site, HYDROLASE, HYDROLASE-INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.95624845742 Å )
Citation :

Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme.

Maianti, J.P.,Tan, G.A.,Vetere, A.  et al.
(2019)  Nat.Chem.Biol.  15 : 565 - 574

PubMed: 31086331
DOI: 10.1038/s41589-019-0271-0

Reaction

Chain : A, B
UniProt : P14735 (IDE_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
Degradation of insulin, glucagon and other polypeptides. No action on proteins. 3.4.24.56 PubMed:10684867, PubMed:17051221, PubMed:17613531, PubMed:18986166, PubMed:19321446, PubMed:21098034, PubMed:2293021, PubMed:23922390, PubMed:24847884, PubMed:26394692, PubMed:29596046
-
Cofactor: Evidence: Note:
Zn(2+) ECO:0000269 | PubMed:17051221
ECO:0000269 | PubMed:18986166
ECO:0000269 | PubMed:19321446
ECO:0000269 | PubMed:21098034
ECO:0000269 | PubMed:23922390
ECO:0000269 | PubMed:26394692
Binds 1 zinc ion per subunit.