proprotein convertase subtilisin/kexin type 1 | S8: Subtilisin | IUPHAR/BPS Guide to PHARMACOLOGY

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proprotein convertase subtilisin/kexin type 1

Target id: 2382

Nomenclature: proprotein convertase subtilisin/kexin type 1

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 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 753 5q15-q21 PCSK1 proprotein convertase subtilisin/kexin type 1
Mouse - 753 13 C2 Pcsk1 proprotein convertase subtilisin/kexin type 1
Rat - 752 2q11-q12 Pcsk1 proprotein convertase subtilisin/kexin type 1
Previous and Unofficial Names
neuroendocrine convertase 1 | prohormone convertase 1 | BDP | NEC1 | PC1 | PC3 | Phpp-1 | prohormone convertase 3 | propeptide-processing protease | SPC3
Database Links
Specialist databases
MEROPS S08.072 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.21.93

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 9.1 pKi 1
pKi 9.1 (Ki 7.5x10-10 M) [1]
Clinically-Relevant Mutations and Pathophysiology
Disease:  Obesity due to prohormone convertase I deficiency
OMIM: 600955, 612362
Orphanet: ORPHA71528

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]

How to cite this page

S8: Subtilisin: proprotein convertase subtilisin/kexin type 1. Last modified on 28/07/2015. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2382.