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proprotein convertase subtilisin/kexin type 5

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Target not currently curated in GtoImmuPdb

Target id: 2385

Nomenclature: proprotein convertase subtilisin/kexin type 5

Family: S8: Subtilisin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1860 9q21.13 PCSK5 proprotein convertase subtilisin/kexin type 5
Mouse 1 1877 19 12.86 cM Pcsk5 proprotein convertase subtilisin/kexin type 5
Rat 1 1809 1q51 Pcsk5 proprotein convertase subtilisin/kexin type 5
Previous and Unofficial Names Click here for help
PC5/6A | PC5A | PC6 | proprotein convertase 5 | proprotein convertase 6 | SPC6
Database Links Click here for help
Specialist databases
MEROPS S08.076 (Hs)
Other databases
Alphafold Q92824 (Hs), Q04592 (Mm), P41413 (Rn)
BRENDA 3.4.21.-
CATH/Gene3D 2.60.120.260, 3.40.50.200
ChEMBL Target CHEMBL2826 (Hs)
Ensembl Gene ENSG00000099139 (Hs), ENSMUSG00000024713 (Mm), ENSRNOG00000012036 (Rn)
Entrez Gene 5125 (Hs), 18552 (Mm), 116548 (Rn)
Human Protein Atlas ENSG00000099139 (Hs)
KEGG Enzyme 3.4.21.-
KEGG Gene hsa:5125 (Hs), mmu:18552 (Mm), rno:116548 (Rn)
OMIM 600488 (Hs)
Pharos Q92824 (Hs)
RefSeq Nucleotide NM_001190482 (Hs), NM_006200 (Hs), NM_001190483 (Mm), NM_053823 (Rn)
RefSeq Protein NP_006191 (Hs), NP_001177411 (Hs), NP_001177412 (Mm), NP_446275 (Rn)
UniProtKB Q92824 (Hs), Q04592 (Mm), P41413 (Rn)
Wikipedia PCSK5 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.-

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pKi 1
⤷ pKi 8.8 (Ki 1.6x10-9 M) [1]
furin inhibitor peptide Peptide Click here for species-specific activity table Hs Inhibition 6.6 pKi 2
⤷ pKi 6.6 (Ki 2.32x10-7 M) [2]
Immuno Process Associations
Immuno Process:  Cytokine production & signalling

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. 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: proprotein convertase subtilisin/kexin type 5. Last modified on 28/07/2015. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2385.