furin, paired basic amino acid cleaving enzyme

Target id: 2366

Nomenclature: furin, paired basic amino acid cleaving enzyme

Family: S8: Subtilisin

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for furin, paired basic amino acid cleaving enzyme in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 794 15q26.1 FURIN furin, paired basic amino acid cleaving enzyme
Mouse - 793 7 D1-E2 Furin furin (paired basic amino acid cleaving enzyme)
Rat - 793 1q31 Furin furin (paired basic amino acid cleaving enzyme)
Previous and Unofficial Names
dibasic-processing enzyme | Fur | PACE | PCSK3 | prohormone convertase 3 | proprotein convertase subtilisin/kexin type 3 | SPC1 | subtilisin pro-protein processing enzyme | furin (paired basic amino acid cleaving enzyme)
Database Links
Specialist databases
MEROPS S08.071 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL 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:  X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba (MI-1148).
PDB Id:  4RYD
Ligand:  MI-1148
Resolution:  2.15Å
Species:  Human
References:  2
Enzyme Reaction
EC Number: 3.4.21.75

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
MI-1148 Hs Inhibition 11.3 pKi 2
pKi 11.3 (Ki 5.5x10-12 M) [2]
phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide Hs Inhibition 9.1 pKi 1
pKi 9.1 (Ki 8.1x10-10 M) [1]
peptide 18 [PMID: 24350995] Hs Inhibition 8.4 pKi 3
pKi 8.4 (Ki 4.3x10-9 M) [3]
furin inhibitor peptide Hs Inhibition 7.6 pKi 4
pKi 7.6 (Ki 2.3x10-8 M) [4]

References

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1. Becker GL, Sielaff F, Than ME, Lindberg I, Routhier S, Day R, Lu Y, Garten W, Steinmetzer T. (2010) Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics. J. Med. Chem.53 (3): 1067-75. [PMID:20038105]

2. Hardes K, Becker GL, Lu Y, Dahms SO, Köhler S, Beyer W, Sandvig K, Yamamoto H, Lindberg I, Walz L et al.. (2015) Novel Furin Inhibitors with Potent Anti-infectious Activity. ChemMedChem10 (7): 1218-31. [PMID:25974265]

3. Kwiatkowska A, Couture F, Levesque C, Ly K, Desjardins R, Beauchemin S, Prahl A, Lammek B, Neugebauer W, Dory YL et al.. (2014) Design, synthesis, and structure-activity relationship studies of a potent PACE4 inhibitor. J. Med. Chem.57 (1): 98-109. [PMID:24350995]

4. Shiryaev SA, Remacle AG, Ratnikov BI, Nelson NA, Savinov AY, Wei G, Bottini M, Rega MF, Parent A, Desjardins R et al.. (2007) Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens. J. Biol. Chem.282 (29): 20847-53. [PMID:17537721]

How to cite this page

S8: Subtilisin: furin, paired basic amino acid cleaving enzyme. Last modified on 30/03/2016. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2366.