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Literature summary for 2.3.2.2 extracted from

  • King, J.B.; West, M.B.; Cook, P.F.; Hanigan, M.H.
    A novel, species-specific class of uncompetitive inhibitors of gamma-glutamyl transpeptidase (2009), J. Biol. Chem., 284, 9059-9065.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.3.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expression in mouse fibroblast Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-chloro-N-[5-(4-chlorobenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-chlorobenzenesulfonamide
-
 Homo sapiens
N-[5-(4-chlorobenzyl)-1,3,4-thiadiazol-2-yl]-4-nitrobenzenesulfonamide
-
 Homo sapiens
N-[5-(4-chlorobenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens
N-[5-(4-methoxybenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide i.e. OU749. Competitive towards glycyclglycine, 150fold less toxic towards dividing cells than inhibitor acivicin. Inhibitory both to enzyme from 786-O cells and to human enzyme expressed in mouse fibroblast Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
RCC 786-O cell ATCC CRL-1932, a GGT-positive renal cell adenocarcinoma line Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-L-glutamyl-4-nitroanilide + Gly-Gly
-
 Homo sapiens 4-nitroaniline + 5-L-glutamyl-Gly-Gly
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0287
-
 4-chloro-N-[5-(4-chlorobenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens
0.0433
-
 N-[5-(4-chlorobenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens
0.0738
-
 N-[5-(4-methoxybenzyl)-1,3,4-thiadiazol-2-yl]benzenesulfonamide
-
 Homo sapiens
0.0743
-
 N-[5-(4-chlorobenzyl)-1,3,4-thiadiazol-2-yl]-4-nitrobenzenesulfonamide
-
 Homo sapiens
0.0759
-
 N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-chlorobenzenesulfonamide
-
 Homo sapiens