Wilk S, Friedman T C, Kline T B
Biochem Biophys Res Commun. 1985 Jul 31;130(2):662-8. doi: 10.1016/0006-291x(85)90468-1.
Pyroglutamyl peptide hydrolase (EC 3.4.11.8), a cysteine protease, cleaves the N-terminal pyroglutamyl residue from pyroglutamyl peptides such as thyrotropin releasing hormone. Pyroglutamyl diazomethyl ketone was synthesized as an active site directed inhibitor. Preincubation of the partially purified bovine brain enzyme with nanomolar concentrations of inhibitor produced rapid inactivation. Inhibitor concentrations five orders of magnitude higher did not inactivate other exo- and endopeptidases. A dose of 0.1 mg/kg administered intraperitoneally to mice totally inactivated the enzyme in all tissues studied including brain. Pyroglutamyl diazomethyl ketone should be of value in studies on the physiological role of this enzyme in the metabolism of pyroglutamyl-containing peptides.
焦谷氨酰肽水解酶（EC 3.4.11.8），一种半胱氨酸蛋白酶，可从焦谷氨酰肽（如促甲状腺激素释放激素）上切割下N端焦谷氨酰残基。合成了焦谷氨酰重氮甲基酮作为活性位点导向抑制剂。用纳摩尔浓度的抑制剂对部分纯化的牛脑酶进行预孵育会导致快速失活。比抑制剂浓度高五个数量级的浓度不会使其他外肽酶和内肽酶失活。给小鼠腹腔注射0.1 mg/kg的剂量会使包括脑在内的所有研究组织中的该酶完全失活。焦谷氨酰重氮甲基酮在研究该酶在含焦谷氨酰肽代谢中的生理作用方面应具有价值。
