Brand  (β version)

PDB ID: 5MIM

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Ligands
Code Name Style Show Link
1N 1-[(1~{R},2~{R},4~{S},5~{S})-2,4-bis(4-carbamimidamidophenoxy)-5-[(4-carbamimidamidophenyl)amino]cyclohexyl]guanidine PoSSuM
CA Calcium ion PoSSuM
CL Chloride ion PoSSuM
NA Sodium ion PoSSuM
Non-standard Residues
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Structure summary

Code : 5MIM   PDBj   RCSB PDB   PDBe
Header : HYDROLASE
Title : Xray structure of human furin bound with the 2,5-dideoxystreptamine derived small molecule inhibitor 1n
Release Data : 2017-05-10
Compound :
mol_id molecule chains synonym
1 Furin A Dibasic-processing enzyme,Paired basic amino acid residue-cleaving enzyme,PACE
ec: 3.4.21.75
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Homo sapiens  (taxid:9606)
gene: FURIN, FUR, PACE, PCSK3
expression_system_common: Human
expression_system_cell_line: HEK293S
Authors : Dahms, S.O., Guan-Sheng, J., Than, M.E.
Keywords : proprotein convertase, inhibitor, protease, complex, hydrolase
Exp. method : X-RAY DIFFRACTION ( 1.900 Å )
Citation :

Structural Studies Revealed Active Site Distortions of Human Furin by a Small Molecule Inhibitor.

Dahms, S.O.,Jiao, G.S.,Than, M.E.
(2017)  ACS Chem. Biol.  12 : 1211 - 1216

PubMed: 28402100
DOI: 10.1021/acschembio.6b01110

Reaction

Chain : A
UniProt : P09958 (FURIN_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
Release of mature proteins from their proproteins by cleavage of -Arg-Xaa-Yaa-Arg-|-Zaa- bonds, where Xaa can be any amino acid and Yaa is Arg or Lys. Releases albumin, complement component C3 and von Willebrand factor from their respective precursors. 3.4.21.75 PubMed:11799113, PubMed:1438214, PubMed:1629222, PubMed:1644824, PubMed:1713771, PubMed:2251280, PubMed:24666235, PubMed:25974265, PubMed:31091448, PubMed:32362314, PubMed:32703818, PubMed:7592877, PubMed:7690548, PubMed:7737999, PubMed:8253774, PubMed:9130696
-
Cofactor: Evidence: Note:
Ca(2+) ECO:0000269 | PubMed:1644824
ECO:0000269 | PubMed:24666235
ECO:0000269 | PubMed:25974265
ECO:0000269 | PubMed:9130696
Binds 3 calcium ions per subunit.