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Literature summary for 3.1.3.48 extracted from

  • Abdjul, D.B.; Yamazaki, H.; Kanno, S.I.; Kirikoshi, R.; Tomizawa, A.; Takahashi, O.; Maarisit, W.; Losung, F.; Rotinsulu, H.; Wewengkang, D.S.; Sumilat, D.A.; Kapojos, M.M.; Namikoshi, M.
    Absolute structures of wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes from aerial parts of Wedelia spp. collected in Indonesia and Japan (2018), Chem. Pharm. Bull., 66, 682-687 .
    View publication on PubMed
Search for more literature for 3.1.3.48

Inhibitors

Inhibitors Comment Organism Structure
(1R,5S,6S,6aR,7S,10S,10aS,11S)-10-(acetyloxy)-7-hydroxy-7,10a-dimethyl-4-methylidene-6-[(2-methylpropanoyl)oxy]-3-oxodecahydro-1H-1,5-methano-2-benzoxocin-11-yl 2-methylprop-2-enoate no inhibition at 0.021 mM Homo sapiens
(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
-
 Homo sapiens
(3aR,4R,4aR,5R,8R,8aR,9S,9aR)-8-(acetyloxy)-5-hydroxy-5,8a-dimethyl-3-methylidene-4-[(2-methylpropanoyl)oxy]-2-oxododecahydronaphtho[2,3-b]furan-9-yl 3-methylbutanoate no inhibition at 0.020 mM Homo sapiens
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylprop-2-enoate no inhibition at 0.025 mM Homo sapiens
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylpropanoate no inhibition at 0.024 mM Homo sapiens
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
-
 Homo sapiens
15-hydroxykaur-9(11),16-dien-19-oic acid
-
 Homo sapiens
3alpha-angeloyloxypterokaurene L3 18% inhibition at 0.024 mM Homo sapiens
3alpha-cinnamoyloxypterokaurene L3
-
 Homo sapiens
3alpha-tigloyloxypterokaurene L3 no inhibition at 0.024 mM Homo sapiens
ent-17-hydroxykaur-15-en-19-oic acid 40% inhibition at 0.033 mM Homo sapiens
ent-3beta-angeloyloxykaur-16-en-19-oic acid
-
 Homo sapiens
ent-3beta-tigloyloxykaur-16-en-19-oic acid
-
 Homo sapiens
ent-kaur-9(11),16-dien-19-oic acid 29% inhibition at 0.033 mM Homo sapiens
additional information wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes, determination and analysis of inhibitors isolated from aerial parts of Wedelia prostrata collected in Manado (Indonesia) and Wedelia chinensis collected on Iriomote Island (Okinawa, Japan). For inhibitory assays, 4-nitrophenyl phosphate is used as enzyme substrate Homo sapiens
oleanolic acid
-
 Homo sapiens
pterokaurene L3 no inhibition at 0.031 mM Homo sapiens
rilobolide-6-O-methacrylate no inhibition at 0.026 mM Homo sapiens
tetrachyrin
-
 Homo sapiens
trilobolide-6-O-isobutyrate no inhibition at 0.026 mM Homo sapiens
wedelolide D 32% inhibition at 0.020 mM Homo sapiens
wedelolide H no inhibition at 0.023 mM Homo sapiens
wedelolide I no inhibition at 0.021 mM Homo sapiens
wedelolide J no inhibition at 0.021 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P18031
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
commercial preparation
-
 Homo sapiens
-
EJ-1 cell
-
 Homo sapiens
-
Huh-7 cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
 Homo sapiens 4-nitrophenol + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
protein tyrosine phosphatase 1B
-
 Homo sapiens
PTP1B
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0011
-
 pH 6.0, 37°C Homo sapiens rilobolide-6-O-methacrylate
0.0077
-
 pH 6.0, 37°C Homo sapiens 3alpha-cinnamoyloxypterokaurene L3
0.0083
-
 pH 6.0, 37°C Homo sapiens (3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
0.012
-
 pH 6.0, 37°C Homo sapiens ent-3beta-angeloyloxykaur-16-en-19-oic acid
0.012
-
 pH 6.0, 37°C Homo sapiens ent-3beta-tigloyloxykaur-16-en-19-oic acid
0.013
-
 pH 6.0, 37°C Homo sapiens 15-hydroxykaur-9(11),16-dien-19-oic acid
0.022
-
 pH 6.0, 37°C Homo sapiens tetrachyrin
0.028
-
 pH 6.0, 37°C Homo sapiens (5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid