Kim Nam Doo, Yoon Jeonghyeok, Kim Jung Ho, Lee Jung Tae, Chon Yong Sog, Hwang Mi-Kyung, Ha Ilho, Song Woo-Joo
Research Center IDRTech Inc., 3rd FL., Chosun Refractory Building, 4-1, Sunae-Dong, Bundang-Ku, Sungnam-Shi, Kyunggi-Do 463-825, South Korea.
Bioorg Med Chem Lett. 2006 Jul 15;16(14):3772-6. doi: 10.1016/j.bmcl.2006.04.042. Epub 2006 May 12.
Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes significant learning and memory deficits in DS-model mice. Thus far, no mechanism-based drug has been developed to address this. After a combination of in silico and in vitro screenings, two DYRK1A inhibitors were isolated that are active in a cell-based assay. Further optimization could lead to a novel drug discovery that could address DS learning and memory deficits.
智力迟钝是唐氏综合征（DS）患者最常见且使人衰弱的病症。过表达导致的DYRK1A过度激活在DS模型小鼠中引起显著的学习和记忆缺陷。迄今为止，尚未开发出基于机制的药物来解决这一问题。经过计算机模拟和体外筛选相结合，分离出两种在细胞试验中具有活性的DYRK1A抑制剂。进一步优化可能会带来一种能够解决DS学习和记忆缺陷的新型药物发现。
