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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and evaluation of dual site inhibitors of 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase.
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Synthesis and evaluation of dual site inhibitors of 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase.

机译：3-脱氧-D-亚硝基庚酸盐7-磷酸合酶双位点抑制剂的合成与评价。

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摘要

3-Deoxy-d-arabino-heptulosonate 7-phosphate (DAH7P) synthase catalyses the first step of the shikimate pathway for the biosynthesis of aromatic compounds. Enzymes of this pathway have been identified as potential targets for drug design. The reaction catalysed by DAH7P synthase is an aldol condensation between phosphoenolpyruvate (PEP) and d-erythrose 4-phosphate (E4P). In this study inhibitors of DAH7P synthase were prepared which were designed to fit into the binding sites of both PEP and E4P substrates simultaneously. Inhibitors, known to target the PEP binding site, were extended using a C4 linker to include an appropriately placed phosphate group in order to access the phosphate-binding site of E4P. A small increase in inhibition was observed with this modification, and the inhibition results have been rationalised by induced-fit docking.
机译：3-脱氧-D-Arabino-庚酸酯7-磷酸盐（DAH7P）合成酶催化Shikimate途径的第一步是芳族化合物的生物合成。 该途径的酶已被鉴定为药物设计的潜在目标。 由DAH7P合成酶催化的反应是磷酸丙酯（PEP）和D-渗碳4-磷酸（E4P）之间的醛醇缩合。 在该研究中，制备DAH7P合酶的抑制剂，其设计成同时配合到两个PEP和E4P基材的结合位点。 使用C4接头延伸以靶向PEP结合位点的抑制剂以包括适当放置的磷酸酯基团，以进入E4P的磷酸盐结合位点。 通过该改性观察到抑制的小幅增加，并且抑制结果通过诱导 - 配合对接合理化。

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