title: Putative therapeutic agents for the learning and memory deficits of people with Down syndrome.
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.
authors.affiliation: Research Center IDRTech Inc., 3rd FL., Chosun Refractory Building, 4-1, Sunae-Dong, Bundang-Ku, Sungnam-Shi, Kyunggi-Do 463-825, South Korea.
authors.forename: Nam Doo
authors.initials: ND
authors.lastname: Kim
authors.forename: Jeonghyeok
authors.initials: J
authors.lastname: Yoon
authors.forename: Jung Ho
authors.initials: JH
authors.lastname: Kim
authors.forename: Jung Tae
authors.initials: JT
authors.lastname: Lee
authors.forename: Yong Sog
authors.initials: YS
authors.lastname: Chon
authors.forename: Mi-Kyung
authors.initials: MK
authors.lastname: Hwang
authors.forename: Ilho
authors.initials: I
authors.lastname: Ha
authors.forename: Woo-Joo
authors.initials: WJ
authors.lastname: Song
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D001665:Binding Sites; D004195:Disease Models, Animal; D004314:Down Syndrome / Q000188:drug therapy* / Q000503:physiopathology; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D006860:Hydrogen Bonding; D007859:Learning Disabilities / Q000188:drug therapy / Q000503:physiopathology; D008569:Memory Disorders / Q000188:drug therapy / Q000503:physiopathology; D051379:Mice; D015394:Molecular Structure; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D000097603:Dyrk Kinases
chemical_list: D000596:Amino Acids; D004791:Enzyme Inhibitors; D017346:Protein Serine-Threonine Kinases; D011505:Protein-Tyrosine Kinases; D000097603:Dyrk Kinases