Kubica Z, Rzeszotarska B, Midura-Nowaczek K, Roszkowska-Jakimiec W
Department of Organic Chemistry, University of Opole, Poland.
Pharmazie. 2000 Nov;55(11):841-4.
Three gamma-glutamyl alpha,beta-dehydroamino acids: L-gamma-glutamyl-dehydroalanine, L-gamma-glutamyl-(Z)-dehydrobutyrine and L-gamma-glutamyl-(E)-dehydrobutyrine have been prepared as potential ligands (inhibitors or substrates) for gamma-glutamyl transpeptidase (GGT). Both isomers of gamma-glutamyl-dehydrobutyrines proved to be inhibitors of GGT, slightly better than the saturated analogue, L-gamma-glutamyl-L-butyrine. However, their solvolysis catalysed by the enzyme is slower than that of the latter. L-gamma-Glutamyl-(E)-dehydrobutyrine seems to be a more active compound in both enzymatic tests. L-gamma-Glutamyl-dehydroalanine elicited only low inhibitory activity and, moreover, was unstable under conditions of the solvolysis test.
三种γ-谷氨酰α,β-脱氢氨基酸：L-γ-谷氨酰脱氢丙氨酸、L-γ-谷氨酰-(Z)-脱氢丁酸和L-γ-谷氨酰-(E)-脱氢丁酸已被制备出来，作为γ-谷氨酰转肽酶（GGT）的潜在配体（抑制剂或底物）。γ-谷氨酰脱氢丁酸的两种异构体均被证明是GGT的抑制剂，略优于饱和类似物L-γ-谷氨酰-L-丁酸。然而，它们在酶催化下的溶剂解比后者慢。在两种酶促试验中，L-γ-谷氨酰-(E)-脱氢丁酸似乎是活性更高的化合物。L-γ-谷氨酰脱氢丙氨酸仅表现出较低的抑制活性，而且在溶剂解试验条件下不稳定。
