二肽基硝基烯烃作为半胱氨酸蛋白酶罗得西亚锥虫蛋白酶和克氏锥虫蛋白酶的强效可逆抑制剂
Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.
作者信息
Latorre Antonio, Schirmeister Tanja, Kesselring Jochen, Jung Sascha, Johé Patrick, Hellmich Ute A, Heilos Anna, Engels Bernd, Krauth-Siegel R Luise, Dirdjaja Natalie, Bou-Iserte Lledó, Rodríguez Santiago, González Florenci V
机构信息
Departament de Química Inorgànica i Orgànica, Universitat Jaume I , 12080 Castelló, Spain.
Institute of Pharmacy and Biochemistry, University of Mainz , Staudinger Weg 5, 55099 Mainz, Germany.
出版信息
ACS Med Chem Lett. 2016 Sep 21;7(12):1073-1076. doi: 10.1021/acsmedchemlett.6b00276. eCollection 2016 Dec 8.
Abstract
Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor resulted to be the most potent one with values of 0.49 and 0.44 nM against rhodesain and cruzain, respectively. According to enzymatic dilution and dialysis experiments, as well as computational and NMR studies, dipeptidyl nitroalkenes are tightly binding covalent reversible inhibitors.
摘要
二肽基硝基烯烃是半胱氨酸蛋白酶的强效可逆抑制剂。抑制剂被证明是最有效的，对罗得西亚锥虫蛋白酶和克氏锥虫蛋白酶的抑制常数分别为0.49和0.44纳摩尔。根据酶稀释和透析实验以及计算和核磁共振研究，二肽基硝基烯烃是紧密结合的共价可逆抑制剂。
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