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Human -Glutamyl Transpeptidase 1: Structures of the Free Enzyme, Inhibitor-Bound Tetrahedral Transition States, and Glutamate-Bound Enzyme Reveal Novel Movement Within the Active Site During Catalysis

Orthogonal validation of NMR fragment hit 27 Encouraged by the relatively high binding affinity of compound 27 compared to expectations for fragments, we synthesised a series of analogues to explore the effect of modifying both the sulfonic acid and the ethoxy substituents on binding affinity (Table 1)

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SL prevented mitochondrial ROS production, cardiolip inoxidation, and citrate carrier failure in cirrhotic livers but did not affect the expression of lipogenic enzymes