Submicromolar phosphinic inhibitors of Escherichia coli aspartate transcarbamoylase |
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| Authors: | Laëtitia Coudray Evan R. Kantrowitz Jean-Luc Montchamp |
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| Affiliation: | 1. Department of Chemistry, Texas Christian University, Box 298860, Fort Worth, TX 76129, USA;2. Department of Chemistry, Boston College, Merkert Chemistry Center, Chestnut Hill, MA 02467-3807, USA |
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| Abstract: | 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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