Putative therapeutic agents for the learning and memory deficits of people with Down syndrome.
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.
Kim
Nam Doo
ND
Research Center IDRTech Inc., 3rd FL., Chosun Refractory Building, 4-1, Sunae-Dong, Bundang-Ku, Sungnam-Shi, Kyunggi-Do 463-825, South Korea.
Yoon
Jeonghyeok
J
Kim
Jung Ho
JH
Lee
Jung Tae
JT
Chon
Yong Sog
YS
Hwang
Mi-Kyung
MK
Ha
Ilho
I
Song
Woo-Joo
WJ
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
D000596:Amino Acids; D004791:Enzyme Inhibitors; D017346:Protein Serine-Threonine Kinases; D011505:Protein-Tyrosine Kinases; D000097603:Dyrk Kinases