Page last updated: 2024-08-07 18:36:35
Prolyl endopeptidase
A prolyl endopeptidase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48147]
Synonyms
PE;
EC 3.4.21.26;
Post-proline cleaving enzyme
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (16.67) | 18.2507 |
| 2000's | 5 (20.83) | 29.6817 |
| 2010's | 13 (54.17) | 24.3611 |
| 2020's | 2 (8.33) | 2.80 |
Compounds (30)
Drugs with Inhibition Measurements
Drugs with Other Measurements
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.Journal of natural products, , 02-22, Volume: 82, Issue:2, 2019
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Inhibition of prolyl oligopeptidase with a synthetic unnatural dipeptide.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
New potent prolyl endopeptidase inhibitors: synthesis and structure-activity relationships of indan and tetralin derivatives and their analogues.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Synthesis and biological evaluation of novel (123)I-labeled 4-(4-iodophenyl)butanoyl-L-prolyl-(2S)-pyrrolidines for imaging prolyl oligopeptidase in vivo.European journal of medicinal chemistry, , May-22, Volume: 79, 2014
Automated parallel synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
New prolyl endopeptidase inhibitors: in vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
New potent prolyl endopeptidase inhibitors: synthesis and structure-activity relationships of indan and tetralin derivatives and their analogues.Journal of medicinal chemistry, , Jun-24, Volume: 37, Issue:13, 1994
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 37, 2021
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).Journal of medicinal chemistry, , Apr-10, Volume: 57, Issue:7, 2014
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.ACS medicinal chemistry letters, , May-09, Volume: 4, Issue:5, 2013
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 59, Issue:9, 2016
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.Journal of medicinal chemistry, , May-13, Volume: 53, Issue:9, 2010
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 18, Issue:15, 2008
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).Journal of medicinal chemistry, , Apr-10, Volume: 57, Issue:7, 2014
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.ACS medicinal chemistry letters, , May-09, Volume: 4, Issue:5, 2013
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| serine-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| serine-type peptidase activity | molecular function | Catalysis of the hydrolysis of peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| oligopeptidase activity | molecular function | Catalysis of the hydrolysis of a peptide bond in an oligopeptide, i.e. a molecule containing a small number (2 to 20) of amino acid residues connected by peptide bonds. [GOC:mah, ISBN:0198506732] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Involved In
This protein is involved in 1 target(s):
| Target | Category | Definition |
|---|
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |