人β-分泌酶（BACE1）的膦基二肽类似物抑制剂的合成及生物学评价
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).
作者信息
Manzenrieder Florian, Frank Andreas O, Huber Timo, Dorner-Ciossek Cornelia, Kessler Horst
机构信息
Department Chemie, Lehrstuhl II für Organische Chemie, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.
出版信息
Bioorg Med Chem. 2007 Jun 15;15(12):4136-43. doi: 10.1016/j.bmc.2007.03.072. Epub 2007 Mar 30.
Phosphino dipeptide (PDP) isosteres are known to be useful analogues of the transition state of metalloprotease substrates. Here we describe the use of this unit for the design of aspartic protease inhibitors. A PDP analogue of OM00-3, a potent BACE1 inhibitor, was synthesized and exhibited high biological activity (IC50 approximately 12 nM).
膦基二肽（PDP）等排体是金属蛋白酶底物过渡态的有用类似物。在此，我们描述了该单元在天冬氨酸蛋白酶抑制剂设计中的应用。合成了强效β-分泌酶1（BACE1）抑制剂OM00-3的一种PDP类似物，其具有高生物活性（半数抑制浓度约为12 nM）。
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