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Carboxylic Acid Amino - Europe PMC

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Last Updated: 16 May 2022

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Rational Design, Synthesis, and Mechanism of (3 S ,4 R )-3-Amino-4-(difluoromethyl)cyclopent-1-ene-1-carboxylic Acid: Employing a Second-Deprotonation Strategy for Selectivity of Human Ornithine Aminotransferase over GABA Aminotransferase.

Human ornithine aminotransferase is a pyridoxal 5'-phosphate-dependent enzyme with a similar active region as -aminobutyric acid aminotransferase. hOAT inhibition has been recently suggested as a potential therapeutic treatment for hepatocellular carcinoma. We first investigated the inactivation mechanisms of hOAT by two well-known GABA-AT inactivators in this research. In the active site of hOAT, the converted Intact protein mass spectrometry, protein crystallography, and dialysis experiments revealed that 10b was converted to an irreversible tight-binding adduct, as had the unsaturated analogue. The active intermediate was only produced in hOAT and not in GABA-AT, according to the comparison of kinetic studies between 10b and 11. The importance of chirality and the endocyclic double bond for inhibitory activity was highlighted by a computational analysis and p K a computational simulations. Mass spectrometric investigation of dissociable products and fluoride ion release experiments supported 10b's turnover mechanism.

Source link: https://europepmc.org/article/MED/35293728

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* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions