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prolyl endopeptidase

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Target not currently curated in GtoImmuPdb

Target id: 2395

Nomenclature: prolyl endopeptidase

Family: S9: Prolyl oligopeptidase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 710 6q21 PREP prolyl endopeptidase
Mouse - 710 10 23.27 cM Prep prolyl endopeptidase
Rat - 710 20q13 Prep prolyl endopeptidase
Previous and Unofficial Names Click here for help
PE | PEP | Pop | post-proline cleaving enzyme
Database Links Click here for help
Specialist databases
MEROPS S09.001 (Hs)
Other databases
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.21.26

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
S 17092 Small molecule or natural product Hs Inhibition 8.8 pKi 1
pKi 8.8 (Ki 1.5x10-9 M) [1]
ARI-3531 Small molecule or natural product Primary target of this compound Hs Inhibition 8.9 pIC50 2
pIC50 8.9 (IC50 1.3x10-9 M) [2]
poststatin Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 3
[3]
Description: IC50 is 0.03 μg/ml in vitro.

References

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1. Lawandi J, Gerber-Lemaire S, Juillerat-Jeanneret L, Moitessier N. (2010) Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors. J Med Chem, 53 (9): 3423-38. [PMID:20058865]

2. Poplawski SE, Lai JH, Li Y, Jin Z, Liu Y, Wu W, Wu Y, Zhou Y, Sudmeier JL, Sanford DG et al.. (2013) Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem, 56 (9): 3467-77. [PMID:23594271]

3. Tsuda M, Muraoka Y, Nagai M, Aoyagi T, Takeuchi T. (1996) Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues. J Antibiot, 49 (9): 890-9. [PMID:8931723]

How to cite this page

S9: Prolyl oligopeptidase: prolyl endopeptidase. Last modified on 05/06/2020. Accessed on 26/10/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2395.