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proprotein convertase subtilisin/kexin type 6

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Target not currently curated in GtoImmuPdb

Target id: 2386

Nomenclature: proprotein convertase subtilisin/kexin type 6

Family: S8: Subtilisin

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 969 15q26.3 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 Click here for help
subtilisin-like proprotein convertase 4 | kexin-like protease PC7A | pace4 | Spc4 | paired basic amino acid cleaving system 4
Database Links Click here for help
Specialist databases
MEROPS S08.075 (Hs)
Other databases
Alphafold P29122 (Hs), Q63415 (Rn)
BRENDA 3.4.21.-
CATH/Gene3D 3.40.50.200, 2.60.120.260
ChEMBL Target CHEMBL2951 (Hs), CHEMBL5507 (Rn)
Ensembl Gene ENSG00000140479 (Hs), ENSMUSG00000030513 (Mm), ENSRNOG00000011526 (Rn)
Entrez Gene 5046 (Hs), 18553 (Mm), 25507 (Rn)
Human Protein Atlas ENSG00000140479 (Hs)
KEGG Enzyme 3.4.21.-
KEGG Gene hsa:5046 (Hs), mmu:18553 (Mm), rno:25507 (Rn)
OMIM 167405 (Hs)
Pharos P29122 (Hs)
RefSeq Nucleotide NM_138325 (Hs), NM_138323 (Hs), NM_138324 (Hs), NM_001291309 (Hs), NM_002570 (Hs), NM_138319 (Hs), NM_138322 (Hs), NM_011048 (Mm), NM_012999 (Rn)
RefSeq Protein NP_002561 (Hs), NP_001278238 (Hs), NP_612192 (Hs), NP_612198 (Hs), NP_612197 (Hs), NP_612196 (Hs), NP_612195 (Hs), NP_035178 (Mm), NP_037131 (Rn)
UniProtKB P29122 (Hs), Q63415 (Rn)
Wikipedia PCSK6 (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 9.2 pKi 1
⤷ pKi 9.2 (Ki 6x10-10 M) [1]
peptide 18 [PMID: 24350995] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pKi 2
⤷ pKi 8.5 (Ki 3.1x10-9 M) [2]
multi-Leu (ML)-peptide Peptide Primary target of this compound Hs Inhibition 7.7 pKi 3
⤷ pKi 7.7 (Ki 1.8x10-8 M) [3]
furin inhibitor peptide Peptide Click here for species-specific activity table 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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2386.