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Submicromolar phosphinic inhibitors of Escherichia coli aspartate transcarbamoylase.

Bioorg Med Chem Lett. 2009 Feb 01;19(3):900-2. Epub 2008 Dec 06
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摘要


The design, syntheses, and enzymatic activity of two submicromolar competitive inhibitors of aspartate transcarbamoylase (ATCase) are described. The phosphinate inhibitors are analogs of N-phosphonacetyl-l-aspartate (PALA) but have a reduced charge at the phosphorus moiety. The mechanistic implications are discussed in terms of a possible cyclic transition-state during enzymatic catalysis.

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