開發針對MraY的核甘抗生素

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開發針對MraY的核甘抗生素

Development of New Nucleoside Antibiotics against Bacterial MraY

馮天佑 , Masters　　Advisor：蒙國光　　

繁體中文

抗生素；抑制劑；卡普拉霉素B ； MraY ； inhibitor ； caprazamycin ； antibiotics

Abstract │ Reference (37) │ Altmetrics

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In this study, we have successfully developed a synthetic approach toward the preparation of structurally complex nucleoside analogues. Based on our strategy, several protecting groups were applied to let us practically prepare these molecules, and the click chemistry was employed to conveniently conjugate a functionalized tag, allowing for the rapidly lipid diversity.
With a general and flexible synthetic approach in hand, we raised three interesting questions: (1) What is the role of chiral center at the C5 position? (2) Is it possible to replace the aminoribose moiety with a simple fragment to shorten the reaction steps? (3) Can we apply a proper functionalized tag to rapidly discover a new and potent lipid moiety in nucleosides to improve its inhibition activity against bacterial MraY?
    In our results toward MraY inhibition study, the chiral center at the C5 position of nucleosides showed only moderate, not dramatic influence to the inhibition potency, Secondly, the structurally complex aminoribose moiety could be replaced with a simple fragment with a five-carbons-chain bearing an amine or guanidine at the end. It may shed a light to develop a new moiety with a more convenient chemistry to accelerate the development of MraY antibiotics. Thirdly, in our nucleoside analogues, the length and structure of the lipid really affected the inhibition potency against MraY. More detail study like a structure activity relationship will be examined in the future. Currently, the best compound showed an approximately 60% inhibition potency against MraY at the concentration at 1 M. Its activity was slightly better than that of natural product, Tunicamycin (46% inhibition) at the same inhibition assay platform.

Reference ( 37 ) 〈TOP〉

1. Abraham, E. P.; Chain, E., An Enzyme from Bacteria able to Destroy Penicillin. Nature 1940, 146, 837‒837
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5. Sykes, R. B.; Bonner, D. P.; Bush, K.; Georgopapadakou, N. H.; Wells, J. S., Monobactams—monocyclic β-lactam antibiotics produced by bacteria. J. Antimicrob. Chemother. 1981, 8, 1‒16.
連結：
14. Bouhss, A.; Mengin-Lecreulx, D.; Le Beller, D.; Van Heijenoort, J., Topological analysis of the MraY protein catalysing the first membrane step of peptidoglycan synthesis. Mol. Microbiol. 1999, 34, 576‒585.
連結：
15. Bouhss, A.; Crouvoisier, M.; Blanot, D.; Mengin-Lecreulx, D., Purification and Characterization of the Bacterial MraY Translocase Catalyzing the First Membrane Step of Peptidoglycan Biosynthesis. J. Med. Chem. 2004, 279, 29974‒29980.
連結：
16. Chung, B. C.; Zhao, J.; Gillespie, R. A.; Kwon, D.-Y.; Guan, Z.; Hong, J.; Zhou, P.; Lee, S.-Y., Crystal Structure of MraY, an Essential Membrane Enzyme for Bacterial Cell Wall Synthesis. Science 2013, 341, 1012‒1016.
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