Literature DB >> 16698266

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

Nam Doo Kim1, Jeonghyeok Yoon, Jung Ho Kim, Jung Tae Lee, Yong Sog Chon, Mi-Kyung Hwang, Ilho Ha, Woo-Joo Song.   

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.

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Year:  2006        PMID: 16698266     DOI: 10.1016/j.bmcl.2006.04.042

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  12 in total

1.  Harmine is an ATP-competitive inhibitor for dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A).

Authors:  Tatyana Adayev; Jerzy Wegiel; Yu-Wen Hwang
Journal:  Arch Biochem Biophys       Date:  2010-12-24       Impact factor: 4.013

Review 2.  Modulating Innate and Adaptive Immunity by (R)-Roscovitine: Potential Therapeutic Opportunity in Cystic Fibrosis.

Authors:  Laurent Meijer; Deborah J Nelson; Vladimir Riazanski; Aida G Gabdoulkhakova; Geneviève Hery-Arnaud; Rozenn Le Berre; Nadège Loaëc; Nassima Oumata; Hervé Galons; Emmanuel Nowak; Laetitia Gueganton; Guillaume Dorothée; Michaela Prochazkova; Bradford Hall; Ashok B Kulkarni; Robert D Gray; Adriano G Rossi; Véronique Witko-Sarsat; Caroline Norez; Frédéric Becq; Denis Ravel; Dominique Mottier; Gilles Rault
Journal:  J Innate Immun       Date:  2016-03-18       Impact factor: 7.349

3.  Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation.

Authors:  Kunal Kumar; Peng Wang; Roberto Sanchez; Ethan A Swartz; Andrew F Stewart; Robert J DeVita
Journal:  J Med Chem       Date:  2018-08-21       Impact factor: 7.446

4.  Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).

Authors:  Andrew S Rosenthal; Cordelle Tanega; Min Shen; Bryan T Mott; James M Bougie; Dac-Trung Nguyen; Tom Misteli; Douglas S Auld; David J Maloney; Craig J Thomas
Journal:  Bioorg Med Chem Lett       Date:  2011-03-04       Impact factor: 2.823

5.  Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity.

Authors:  Kunal Kumar; Peter Man-Un Ung; Peng Wang; Hui Wang; Hailing Li; Mary K Andrews; Andrew F Stewart; Avner Schlessinger; Robert J DeVita
Journal:  Eur J Med Chem       Date:  2018-08-22       Impact factor: 6.514

6.  Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).

Authors:  Bryan T Mott; Cordelle Tanega; Min Shen; David J Maloney; Paul Shinn; William Leister; Juan J Marugan; James Inglese; Christopher P Austin; Tom Misteli; Douglas S Auld; Craig J Thomas
Journal:  Bioorg Med Chem Lett       Date:  2009-10-03       Impact factor: 2.823

Review 7.  Function and regulation of Dyrk1A: towards understanding Down syndrome.

Authors:  Joongkyu Park; Woo-Joo Song; Kwang Chul Chung
Journal:  Cell Mol Life Sci       Date:  2009-08-14       Impact factor: 9.261

Review 8.  Recent advances in the design, synthesis, and biological evaluation of selective DYRK1A inhibitors: a new avenue for a disease modifying treatment of Alzheimer's?

Authors:  Breland Smith; Federico Medda; Vijay Gokhale; Travis Dunckley; Christopher Hulme
Journal:  ACS Chem Neurosci       Date:  2012-08-28       Impact factor: 4.418

9.  Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.

Authors:  Kunal Kumar; Peng Wang; Jessica Wilson; Viktor Zlatanic; Cecilia Berrouet; Susmita Khamrui; Cody Secor; Ethan A Swartz; Michael Lazarus; Roberto Sanchez; Andrew F Stewart; Adolfo Garcia-Ocana; Robert J DeVita
Journal:  J Med Chem       Date:  2020-02-19       Impact factor: 7.446

10.  Hologram QSAR models of a series of 6-arylquinazolin-4-amine inhibitors of a new Alzheimer's disease target: dual specificity tyrosine-phosphorylation-regulated kinase-1A enzyme.

Authors:  Felipe Dias Leal; Camilo Henrique da Silva Lima; Ricardo Bicca de Alencastro; Helena Carla Castro; Carlos Rangel Rodrigues; Magaly Girão Albuquerque
Journal:  Int J Mol Sci       Date:  2015-03-06       Impact factor: 5.923

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