强效且高选择性的人β-分泌酶2（膜内天冬氨酸蛋白酶1）抑制剂的设计，2型糖尿病的一个靶点
Design of Potent and Highly Selective Inhibitors for Human β-Secretase 2 (Memapsin 1), a Target for Type 2 Diabetes.
作者信息
Ghosh Arun K, Reddy Bhavanam Sekhara, Yen Yu-Chen, Cardenas Emilio, Rao Kalapala Venketeswara, Downs Deborah, Huang Xiangping, Tang Jordan, Mesecar Andrew D
机构信息
Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907 (USA).
Department of Biological Sciences, Purdue University, West Lafayette, IN 47907 (USA).
出版信息
Chem Sci. 2016 May 1;7(5):3117-3122. doi: 10.1039/C5SC03718B. Epub 2016 Feb 4.
Design, synthesis and evaluation of very potent and selective β-Secretase 2 (memapsin 1, BACE 2) inhibitors are described. The inhibitors were designed specifically to interact with the S2'-site of β-secretase 2 to provide >170,000-fold selectivity over β-secretase (BACE 1) and >15,000-fold selectivity over cathepsin D. BACE 2 is implicated in Type 2 diabetes. The studies serve as an important guide to selective BACE 2 inhibitors.
本文描述了强效且选择性的β-分泌酶2（膜天冬氨酸蛋白酶1，BACE 2）抑制剂的设计、合成及评估。这些抑制剂经专门设计，可与β-分泌酶2的S2'-位点相互作用，对β-分泌酶（BACE 1）的选择性大于170,000倍，对组织蛋白酶D的选择性大于15,000倍。BACE 2与2型糖尿病有关。这些研究为选择性BACE 2抑制剂提供了重要指导。
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