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Synthesis and evaluation of a mechanism-based inhibitor of KDO8P synthase by Valery Belakhov; Ekaterina Dovgolevsky; Emilia Rabkin; Smadar Shulami; Yuval Shoham; Timor Baasov is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthesis and evaluation of a mechanism-based inhibitor of KDO8P synthase about?
The enzyme 3-deoxy-D D -manno-2-octulosonate-8-phosphate (KDO8P) synthase catalyzes the condensation reaction between phosphoenolpyruvate (PEP) and D D -arabinose 5-phosphate (A5P) to produce KDO8P and inorganic phosphate. In attempts to investigate the lack of antibacterial activity of the most potent inhibitor of KDO8P synthase, the amino phosphonophosphate 3, we have synthesized its hydrolytically stable isosteric phosphonate analogue 4 and tested it as an inhibitor of the enzyme. The synthesis of 4 was accomplished in a one step procedure by employing the direct reductive amination in aqueous media between unprotected sugar phosphonate and glyphosate. The analogue 4 proved to be a competitive inhibitor of KDO8P synthase with respect to both substrates A5P and PEP binding. In vitro antibacterial tests against a series of different Gram-negative organisms establish that both inhibitors (3 and 4) lack antibacterial activity probably due to their reduced ability to penetrate the bacterial cell membrane.
Who reads Synthesis and evaluation of a mechanism-based inhibitor of KDO8P synthase?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Valery Belakhov; Ekaterina Dovgolevsky; Emilia Rabkin; Smadar Shulami; Yuval Shoham; Timor Baasov
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0008-6215)
- Published
- 2004
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)