proprotein convertase subtilisin/kexin type 6

Target id: 2386

Nomenclature: proprotein convertase subtilisin/kexin type 6

Family: S8: Subtilisin

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for proprotein convertase subtilisin/kexin type 6 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 969 15q26 PCSK6 proprotein convertase subtilisin/kexin type 6
Mouse - 959 7 C Pcsk6 proprotein convertase subtilisin/kexin type 6
Rat - 937 1q22 Pcsk6 proprotein convertase subtilisin/kexin type 6
Previous and Unofficial Names
subtilisin-like proprotein convertase 4 | kexin-like protease PC7A | pace4 | Spc4 | paired basic amino acid cleaving system 4
Database Links
Specialist databases
MEROPS S08.075 (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
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.21.-

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
phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide Hs Inhibition 9.2 pKi 1
pKi 9.2 (Ki 6x10-10 M) [1]
peptide 18 [PMID: 24350995] Hs Inhibition 8.5 pKi 2
pKi 8.5 (Ki 3.1x10-9 M) [2]
multi-Leu (ML)-peptide Hs Inhibition 7.7 pKi 3
pKi 7.7 (Ki 1.8x10-8 M) [3]
furin inhibitor peptide Hs Inhibition 6.8 pKi 4
pKi 6.8 (Ki 1.62x10-7 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. 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]

3. Levesque C, Fugère M, Kwiatkowska A, Couture F, Desjardins R, Routhier S, Moussette P, Prahl A, Lammek B, Appel JR et al.. (2012) The Multi-Leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells. J. Med. Chem.55 (23): 10501-11. [PMID:23126600]

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: proprotein convertase subtilisin/kexin type 6. Last modified on 28/07/2015. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2386.