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4, 4-Difluorinated analogues of l-arginine and N G-hydroxy-l-arginine as mechanistic probes for nitric oxide synthase

…, JJ Woodward, MB Winter, MA Marletta

文献索引:Martin, Nathaniel I.; Woodward, Joshua J.; Winter, Michael B.; Marletta, Michael A. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1758 - 1762

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被引用次数: 5

摘要

4, 4-Difluoro-l-arginine and 4, 4-difluoro-NG-hydroxy-l-arginine were synthesized and shown to be substrates for the inducible isoform of nitric oxide synthase (iNOS). Binding of both fluorinated analogues to the NOS active site was also investigated using a spectral binding assay employing a heme domain construct of the inducible NOS isoform (iNOSheme). 4, 4-Difluoro-NG-hydroxy-arginine was found to bind at the NOS active site ...