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prolyl endopeptidase

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Target id: 2395

Nomenclature: prolyl endopeptidase

Family: S9: Prolyl oligopeptidase

Contents:

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 P48147 (Hs), Q9QUR6 (Mm), O70196 (Rn)
BRENDA 3.4.21.26
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL3202 (Hs), CHEMBL4935 (Mm), CHEMBL4035 (Rn)
Ensembl Gene ENSG00000085377 (Hs), ENSMUSG00000019849 (Mm), ENSRNOG00000051061 (Rn)
Entrez Gene 5550 (Hs), 19072 (Mm), 83471 (Rn)
Human Protein Atlas ENSG00000085377 (Hs)
KEGG Enzyme 3.4.21.26
KEGG Gene hsa:5550 (Hs), mmu:19072 (Mm), rno:83471 (Rn)
OMIM 600400 (Hs)
Pharos P48147 (Hs)
RefSeq Nucleotide NM_002726 (Hs), NM_011156 (Mm), NM_031324 (Rn)
RefSeq Protein NP_002717 (Hs), NP_035286 (Mm), NP_112614 (Rn)
UniProtKB P48147 (Hs), Q9QUR6 (Mm), O70196 (Rn)
Wikipedia PREP (Hs)
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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2395.