Synthesis and evaluation of novel dipeptide-bound 1, 2, 4-thiadiazoles as irreversible inhibitors of guinea pig liver transglutaminase

C Marrano, P de Macédo, P Gagnon, D Lapierre…

文献索引：Marrano; de Macedo; Gagnon; Lapierre; Gravel; Keillor Bioorganic and medicinal chemistry, 2001 , vol. 9, # 12 p. 3231 - 3241

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被引用次数: 53

摘要

Herein we report the synthesis and evaluation of 14 novel peptides as potential irreversible inactivators of guinea pig liver transglutaminase (TGase). These peptides were designed to resemble Cbz-l-Gln-Gly, known to be a good TGase substrate, and to include a 1, 2, 4- thiadiazole group. The side chain length of the amino acid residue bearing the inhibitor group was also varied in order to permit investigation of this effect. Their inactivation rate ...