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Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 1 | 794 | 15q26.1 | FURIN | furin, paired basic amino acid cleaving enzyme | |
| Mouse | 1 | 793 | 7 45.65 cM | Furin | furin, paired basic amino acid cleaving enzyme | |
| Rat | 1 | 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 |
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| Specialist databases | |
| MEROPS | S08.071 (Hs) |
| Other databases | |
| Alphafold | P09958 (Hs), P23188 (Mm), P23377 (Rn) |
| BRENDA | 3.4.21.75 |
| CATH/Gene3D | 2.60.120.260, 3.40.50.200 |
| ChEMBL Target | CHEMBL2611 (Hs) |
| Ensembl Gene | ENSG00000140564 (Hs), ENSMUSG00000030530 (Mm), ENSRNOG00000011352 (Rn) |
| Entrez Gene | 5045 (Hs), 18550 (Mm), 54281 (Rn) |
| Human Protein Atlas | ENSG00000140564 (Hs) |
| KEGG Enzyme | 3.4.21.75 |
| KEGG Gene | hsa:5045 (Hs), mmu:18550 (Mm), rno:54281 (Rn) |
| OMIM | 136950 (Hs) |
| Pharos | P09958 (Hs) |
| RefSeq Nucleotide | NM_002569 (Hs), NM_001081454 (Mm), NM_011046 (Mm), NM_019331 (Rn) |
| RefSeq Protein | NP_002560 (Hs), NP_035176 (Mm), NP_001074923 (Mm), NP_062204 (Rn) |
| SynPHARM | 82448 (in complex with MI-1148) |
| UniProtKB | P09958 (Hs), P23188 (Mm), P23377 (Rn) |
| Wikipedia | FURIN (Hs) |
| Selected 3D Structures |
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| Enzyme Reaction |
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Inhibitor Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| The furin inhibitor decanoyl-RVKR-chloromethylketone inhibits cleavage of SARS-CoV-2 spike glycoprotein at the furin cleavage site, and this partially inhibits the capacity of the virus to infect host cells [2]. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Immuno Process Associations | ||
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| General Comments |
| Several viruses exploit the serine peptidase activity of furin to activate their envelope glycoproteins, to facilitate fusion of their membranes with host cell membranes during the infection process [3]. Specific viruses that utilise host furin include HIV-1 [4] and SARS-CoV-2 [2]. Application of furin inhibitors in vitro can block infection by these viruses, and reduce viral replicative capacity. |
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. Cheng Y-W, Chao T-L, Li C-L, Chen P-J, Chang S-Y, Yeh S-H. (2020) Furin Inhibitors Block SARS-CoV-2 Spike Protein Cleavage to Suppress Virus Production and Cytopathic Effects. Cell Reports, [Epub ahead of print]. DOI: 10.1016/j.celrep.2020.108254
3. Gagnon H, Beauchemin S, Kwiatkowska A, Couture F, D'Anjou F, Levesque C, Dufour F, Desbiens AR, Vaillancourt R, Bernard S et al.. (2014) Optimization of furin inhibitors to protect against the activation of influenza hemagglutinin H5 and Shiga toxin. J Med Chem, 57 (1): 29-41. [PMID:24359257]
4. Hallenberger S, Bosch V, Angliker H, Shaw E, Klenk HD, Garten W. (1992) Inhibition of furin-mediated cleavage activation of HIV-1 glycoprotein gp160. Nature, 360 (6402): 358-61. [PMID:1360148]
5. 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. ChemMedChem, 10 (7): 1218-31. [PMID:25974265]
6. 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]
7. 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]
S8: Subtilisin: furin, paired basic amino acid cleaving enzyme. Last modified on 25/09/2020. Accessed on 26/01/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2366.
