Putative therapeutic agents for the learning and memory deficits of people with Down syndrome

  • Bioorg Med Chem Lett. 2006 Jul 15;16(14):3772-6. doi: 10.1016/j.bmcl.2006.04.042.
Nam Doo Kim  1 Jeonghyeok Yoon Jung Ho Kim Jung Tae Lee Yong Sog Chon Mi-Kyung Hwang Ilho Ha Woo-Joo Song
Affiliations
  • 1. Research Center IDRTech Inc., 3rd FL., Chosun Refractory Building, 4-1, Sunae-Dong, Bundang-Ku, Sungnam-Shi, Kyunggi-Do 463-825, South Korea.
Abstract

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.