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Literature summary for 3.4.22.1 extracted from

  • Cunha, R.L.; Gouvea, I.E.; Feitosa, G.P.; Alves, M.F.; Broemme, D.; Comasseto, J.V.; Tersariol, I.L.; Juliano, L.
    Irreversible inhibition of human cathepsins B, L, S and K by hypervalent tellurium compounds (2009), Biol. Chem., 390, 1205-1212.
    View publication on PubMed

Application

Application Comment Organism
drug development cathepsin B is a target for development of efficient and specific inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-3-chloro-1-phenyl-2-(trichloro-lambda4-tellanyl)prop-2-en-1-ol
-
Homo sapiens
(2Z)-1,3-bis(2-methoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
Homo sapiens
(2Z)-1,3-bis(4-ethoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
Homo sapiens
(2Z)-1,3-bis(4-methoxyphenyl)-4-(trichloro-lambda4-tellanyl)but-2-en-1-one
-
Homo sapiens
(2Z)-1,3-diphenyl-4-(trichloro-llambda4-tellanyl)but-2-en-1-one
-
Homo sapiens
(3E)-2-bromo-3-(bromomethylidene)-2-(4-methoxyphenyl)-1-oxa-2l4-telluraspiro[3.5]nonane
-
Homo sapiens
(3E)-2-chloro-3-(chloromethylidene)-2-(4-methoxyphenyl)-1-oxa-2l4-telluraspiro[3.5]nonane
-
Homo sapiens
(3E)-4-chloro-3-[dichloro(4-methoxyphenyl)-l4-tellanyl]-2-methylbut-3-en-2-ol
-
Homo sapiens
1,1,3-trichloro-2,4,5,6-tetrahydro-1H-1-benzotellurophene
-
Homo sapiens
1-(dichloro[(1E)-1-chloro-3-methoxyprop-1-en-2-yl]-l4-tellanyl)-4-methoxybenzene
-
Homo sapiens
1-(dichloro[(Z)-2-chloro-2-phenylethenyl]-l4-tellanyl)-4-methoxybenzene bis-vinylic organotellurane, can be a candidate as a starting compound to design more efficient and specific inhibitors for cathepsin B Homo sapiens
2-[(6-([3'-(aminomethyl)biphenyl-3-yl]oxy)-3,5-difluoropyridin-2-yl)oxy]benzoic acid
-
Homo sapiens
ammonium 1-tribromo-1,3,2-dioxatellurolane
-
Homo sapiens
ammonium 1-trichloro-1,3,2-dioxatellurolane
-
Homo sapiens
additional information design and synthesis of hypervalent tellurium compounds, and irreversible inhibition of cathepsins B by hypervalent tellurium compounds, e.g. organotellurium(IV) compounds, i.e. organotelluranes, that react with thiols forming mixed dichalcogenides, with a tellurium-sulfur bond. Mechanisms for two- and one-step irreversible enzyme inhibition, overview Homo sapiens
N-benzyl-N,N-diethylethanaminium 1-trichloro-4-chloro-2,3-dihydro-2-oxatellurophene
-
Homo sapiens
trichloro(dioxoethylene-O,O')tellurate
-
Homo sapiens
[N-benzyl-N,N-diethylethanaminium]2 hexachloro-lambda6-tellane
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
-
Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information second-order inactivation rate constants for cathepsin B, overview Homo sapiens
0.0127
-
ammonium 1-trichloro-1,3,2-dioxatellurolane pH 6.5, 25°C Homo sapiens
0.0302
-
ammonium 1-tribromo-1,3,2-dioxatellurolane pH 6.5, 25°C Homo sapiens
0.1675
-
[N-benzyl-N,N-diethylethanaminium]2 hexachloro-lambda6-tellane pH 6.5, 25°C Homo sapiens