Submicromolar phosphinic inhibitors of Escherichia coli aspartate transcarbamoylase

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:19

Article

Coudray, Laetitia¹  Kantrowitz, Evan R.²  Montchamp, Jean-Luc¹ 

[1] Texas Christian Univ, Dept Chem, Ft Worth, TX 76129 USA

[2] Boston Coll, Dept Chem, Merkert Chem Ctr, Chestnut Hill, MA 02467 USA

关键词: Enzyme inhibitor;    Aspartate transcarbamoylase;    Phosphinate;    Phosphonate;   

DOI  :  10.1016/j.bmcl.2008.11.115

来源: Elsevier

【 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. (C) 2008 Elsevier Ltd. All rights reserved.

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