Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology and Chemistry, Vanderbilt University Medical Center, Vanderbilt University , Nashville, Tennessee 37232-6600, United States.
ACS Chem Neurosci. 2012 Jan 18;3(1):3-4. doi: 10.1021/cn200124u.
A "second generation" γ-secretase, Begacestat (GSI-953), which is more selective against Notch-signaling, has shown promise in recent Phase I clinical trials. Begacestat, a novel, 2,5-disubsitituted thiophene sulfonamide from Wyeth (now Pfizer) is under evaluation for the treatment of Alzheimer's disease.
一种“第二代”γ-分泌酶，贝卡斯特（GSI-953），对 Notch 信号具有更高的选择性，在最近的 I 期临床试验中显示出了前景。贝卡斯特是惠氏（现为辉瑞）的一种新型 2,5-二取代噻吩磺酰胺，正在评估用于治疗阿尔茨海默病。
