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Literature summary extracted from

  • Lawandi, J.; Toumieux, S.; Seyer, V.; Campbell, P.; Thielges, S.; Juillerat-Jeanneret, L.; Moitessier, N.
    Constrained peptidomimetics reveal detailed geometric requirements of covalent prolyl oligopeptidase inhibitors (2009), J. Med. Chem., 52, 6672-6684.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.26 benzyl [(2R)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate 0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [(2R,3R,7aS)-3-cyano-2-methyl-5-oxohexahydropyrrolo[2,1-b][1,3]oxazol-6-yl]carbamate 0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from brain-derived endothelial cells, more than 50% inhibition in extracts from brain-derived endothelial cells Homo sapiens
3.4.21.26 benzyl [(2S)-1-[(2S)-2-cyanopyrrolidin-1-yl]-1-oxopropan-2-yl]carbamate 0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [(3R,6R,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate 0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [(3R,6R,8aS)-3-cyano-5-oxohexahydro-5H-[1,3]thiazolo[3,2-a]pyridin-6-yl]carbamate 0.1 mM, more than 50% inhibition in extracts from astrocyte-derived cells, extracts from brain-derived endothelial cells and extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [(3R,6S,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate 0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from brain-derived endothelial cells, more than 50% inhibition in extracts from brain-derived endothelial cells Homo sapiens
3.4.21.26 benzyl [(3R,6S,8aS)-3-cyano-5-oxohexahydro-5H-[1,3]thiazolo[3,2-a]pyridin-6-yl]carbamate 0.1 mM, more than 50% inhibition in extracts from astrocyte-derived cells, extracts from brain-derived endothelial cells and extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [(3R,7aS)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]oxazol-6-yl]carbamate 0.1 mM, 10-50% inhibition in extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [(3S,6R,7aR)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate 0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from brain-derived endothelial cells, more than 50% inhibition in extracts from brain-derived endothelial cells Homo sapiens
3.4.21.26 benzyl [(3S,6S,7aR)-3-cyano-5-oxohexahydropyrrolo[2,1-b][1,3]thiazol-6-yl]carbamate 0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and brain-derived endothelial cells Homo sapiens
3.4.21.26 benzyl [(4S,7S,8aS)-4-cyano-6-oxohexahydro-2H-pyrrolo[2,1-b][1,3]thiazin-7-yl]carbamate 0.1 mM, 10-50% inhibition in extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [2-(2-cyanopiperidin-1-yl)-2-oxoethyl]carbamate 0.1 mM, 10-50% inhibition in extracts from brain-derived endothelial cells and extracts from fibroblasts, more than 50% inhibition in extracts from astrocyte-derived cells Homo sapiens
3.4.21.26 benzyl [2-[(2R)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate 0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens
3.4.21.26 benzyl [2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamate 0.02 mM, more than 90% inhibition in extracts from brain-derived endothelial cells, extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens
3.4.21.26 Cbz-Pro-CN 0.1 mM, 10-50% inhibition in extracts from brain-derived endothelial cells Homo sapiens
3.4.21.26 Cbz-Pro-NH2 0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens
3.4.21.26 methyl (3R,6R,7aS)-6-[[(benzyloxy)carbonyl]amino]-5-oxohexahydropyrrolo[2,1-b][1,3]thiazole-3-carboxylate 0.1 mM, 10-50% inhibition in extracts from fibroblasts Homo sapiens
3.4.21.26 methyl (3R,6S,7aS)-6-[[(benzyloxy)carbonyl]amino]-5-oxohexahydropyrrolo[2,1-b][1,3]thiazole-3-carboxylate 0.1 mM, 10-50% inhibition in extracts from astrocyte-derived cells and extracts from fibroblasts Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.14.5 Homo sapiens
-
-
-
3.4.21.26 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.14.5 endothelial cell line HCEC Homo sapiens
-
3.4.14.5 fibroblast lung-derived and skin-derived Homo sapiens
-
3.4.14.5 glioblastoma cell
-
 Homo sapiens
-
3.4.21.26 endothelial cell line HCEC Homo sapiens
-
3.4.21.26 fibroblast lung-derived and skin-derived Homo sapiens
-
3.4.21.26 glioblastoma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.14.5 Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.21.26 Z-Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens z-Gly-Pro + 7-amino-4-methylcoumarin
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.14.5 DPP IV
-
 Homo sapiens
3.4.14.5 prolyl-dipeptidyl-aminopeptidase
-
 Homo sapiens
3.4.21.26 POP
-
 Homo sapiens
3.4.21.26 prolyl oligopeptidase
-
 Homo sapiens