Synthesis and characterization of intermediate and transition-state analogue inhibitors of gamma-glutamyl peptide ligases |
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Authors: | Inoue M Hiratake J Sakata K |
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Affiliation: | Institute for Chemical Research, Kyoto University, Japan. |
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Abstract: | The phosphonodifluoromethyl ketone and phosphonofluoridate derivatives of L-glutamic acid were synthesized and characterized as analogues of the gamma-glutamyl phosphate intermediate and the tetrahedral transition state, respectively, for the inhibition of gamma-glutamylcysteine synthetase and glutamine synthetase. The former served as a poor inhibitor of both enzymes, but the latter inhibited glutamine synthetase with a Ki of 59 microM and partially inactivated the enzyme in an NH3- and ATP-dependent manner. |
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