- Freezing the Dynamic Gap for Selectivity: Motion-Based Design of Inhibitors of the Shikimate Kinase Enzyme
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Shikimate kinase (SK), the fifth enzyme of the aromatic amino acid biosynthesis, is a recognized target for antibiotic drug discovery. The potential of the distinct dynamic apolar gap, which isolates the natural substrate from the solvent environment for
- Prado, Verónica,Lence, Emilio,Thompson, Paul,Hawkins, Alastair R.,González-Bello, Concepción
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- Synthesis and evaluation of two new inhibitors of EPSP synthase
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The enzyme EPSP synthase, EPSPS, (EC 2.5.1.19) catalyzes an unusual transfer reaction of the enolpyruvoyl moiety from phosphoenol pyruvate (2, PEP) regiospecifically to the 5-OH of shikimate 3-phosphate (1, S3P) to form 5-enol-pyruvoylshikimate 3-phosphate (3, EPSP). Two new inhibitors, (4, and 5) were prepared to probe the S3P binding site.
- Pansegrau, Paul D.,Anderson, Karen S.,Widlanski, Theodore,Ream, Joel E.,Douglas Sammons,Sikorski, James A.,Knowles, Jeremy R.
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p. 2589 - 2592
(2007/10/02)
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