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Literature summary for 3.4.21.26 extracted from

  • Lee, S.H.; Jun, M.; Choi, J.Y.; Yang, E.J.; Hur, J.M.; Bae, K.; Seong, Y.H.; Huh, T.L.; Song, K.S.
    Plant phenolics as prolyl endopeptidase inhibitors (2007), Arch. Pharm. Res., 30, 827-833.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1,2,3,4,6-pentagalloyl glucopyranoside specific, noncompetitive, and strong inhibition Homo sapiens
1,2,3,6-tetragalloyl alloside specific, noncompetitive, and strong inhibition Homo sapiens
1,2,3-trigalloyl glucopyranoside specific, noncompetitive, and strong inhibition Homo sapiens
1,2,6-trigalloyl alloside specific, noncompetitive, and strong inhibition Homo sapiens
1,2,6-trigalloyl glucopyranoside from Euphorbia helioscopia, specific, noncompetitive, and strong inhibition Homo sapiens
1,3,6-trigalloyl alloside specific, noncompetitive, and strong inhibition Homo sapiens
acetonyl geraniin specific, noncompetitive, and strong inhibition Homo sapiens
bixanin specific and noncompetitive inhibition Homo sapiens
corilagin specific, noncompetitive, and strong inhibition Homo sapiens
elaeocarpusin specific, noncompetitive, and strong inhibition Homo sapiens
euphorscopin specific, noncompetitive, and strong inhibition Homo sapiens
geraniin specific, noncompetitive, and strong inhibition Homo sapiens
ginkgolic acid
-
Homo sapiens
helioscopin B specific, noncompetitive, and strong inhibition Homo sapiens
helioscopinin A specific, noncompetitive, and strong inhibition Homo sapiens
helioscopinin B specific, noncompetitive, and strong inhibition Homo sapiens
jolkinin specific, noncompetitive, and strong inhibition Homo sapiens
kinapsin-24
-
Homo sapiens
macranganin from Euphorbia fisheriana, specific, noncompetitive, and strong inhibition Homo sapiens
additional information at least 3 galloyl groups are required for strong inhibition activity by Euphorbiaceae plants, poor inhibition by 1-galloyl glucopyranoside, 1,6-digalloyl glucopyranoside, 2,6-digalloyl glucopyranoside, 2-galloyl galactose, 6-galloyl-1-O-(4-gallate)-glucopyranoside, 6-galloyl-1-O-(phloroglucinol)-glucopyranoside, gallic acid, furosin, anthricin, gomisin A, tigloyl gomisin, 8-C-(glucopyranosyl)-kaempferol, 3-O-galloyl shikimate, 4-O-galloyl shikimate, 3-O-(2-galloyl-glucopyranosyl)-quercetin, quercetin-3-O-glucopyranoside, alpha-viniferin, 5-O-galloylquininc acid, and shizarin, overview Homo sapiens
N-benzyloxycarbonyl-L-prolyl-L-prolinal i.e. Z-Pro-prolinal Homo sapiens
rugosin E from Euphorbia supina, specific, noncompetitive, and strong inhibition Homo sapiens
staurosporine
-
Homo sapiens
supinanin specific, noncompetitive, and strong inhibition Homo sapiens
teracatain specific, noncompetitive, and strong inhibition Homo sapiens
Z-Pro-prolinal
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain of Alzheimer's disease patients, showing high enzyme expression levels, and healthy individuals Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-succinyl-Ala-Ala-Ala-4-nitroanilide
-
Homo sapiens N-succinyl-Ala-Ala-Ala + 4-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
prolyl endopeptidase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000004
-
1,3,6-trigalloyl alloside
-
Homo sapiens
0.0000046
-
euphorscopin
-
Homo sapiens
0.0000094
-
rugosin E
-
Homo sapiens
0.0000171
-
geraniin
-
Homo sapiens
0.0000184
-
elaeocarpusin
-
Homo sapiens
0.0000194
-
1,2,6-trigalloyl glucopyranoside
-
Homo sapiens
0.0000272
-
1,2,3,4,6-pentagalloyl glucopyranoside
-
Homo sapiens
0.000074
-
acetonyl geraniin
-
Homo sapiens
0.000091
-
supinanin
-
Homo sapiens
0.000098
-
helioscopinin B
-
Homo sapiens
0.000102
-
helioscopinin A
-
Homo sapiens
0.000129
-
helioscopin B
-
Homo sapiens
0.000194
-
1,2,6-trigalloyl glucopyranoside
-
Homo sapiens
0.000203
-
1,2,6-trigalloyl alloside
-
Homo sapiens
0.000212
-
corilagin
-
Homo sapiens
0.000405
-
1,2,3,6-tetragalloyl alloside
-
Homo sapiens
0.000441
-
macranganin
-
Homo sapiens
0.00079
-
jolkinin
-
Homo sapiens
0.001717
-
teracatain
-
Homo sapiens
0.00249
-
1,2,3-trigalloyl glucopyranoside
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000267
-
-
Homo sapiens rugosin E
0.0000314
-
-
Homo sapiens 1,2,6-trigalloyl glucopyranoside
0.0000426
-
-
Homo sapiens macranganin
0.0000516
-
-
Homo sapiens Z-Pro-prolinal
0.00062
-
-
Homo sapiens ginkgolic acid
0.00077
-
-
Homo sapiens staurosporine
0.00114
-
-
Homo sapiens kinapsin-24
0.0231
-
-
Homo sapiens bixanin