Literature DB >> 21450467

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

Andrew S Rosenthal1, Cordelle Tanega, Min Shen, Bryan T Mott, James M Bougie, Dac-Trung Nguyen, Tom Misteli, Douglas S Auld, David J Maloney, Craig J Thomas.   

Abstract

Continued examination of substituted 6-arylquinazolin-4-amines as Clk4 inhibitors resulted in selective inhibitors of Clk1, Clk4, Dyrk1A and Dyrk1B. Several of the most potent inhibitors were validated as being highly selective within a comprehensive kinome scan. Published by Elsevier Ltd.

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Year:  2011        PMID： 21450467      PMCID： PMC3085634          DOI： 10.1016/j.bmcl.2011.02.114

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


  39 in total

Review 1.  Pre-mRNA splicing and human disease.

Authors:  Nuno André Faustino; Thomas A Cooper
Journal:  Genes Dev       Date:  2003-02-15       Impact factor: 11.361

2.  Mirk/Dyrk1B, a novel therapeutic target, mediates cell survival in non-small cell lung cancer cells.

Authors:  Jingchun Gao; Zhong Zheng; Bhupendra Rawal; Michael J Schell; Gerold Bepler; Eric B Haura
Journal:  Cancer Biol Ther       Date:  2009-09-20       Impact factor: 4.742

3.  Regulation of alternative splicing of human tau exon 10 by phosphorylation of splicing factors.

Authors:  A M Hartmann; D Rujescu; T Giannakouros; E Nikolakaki; M Goedert; E M Mandelkow; Q S Gao; A Andreadis; S Stamm
Journal:  Mol Cell Neurosci       Date:  2001-07       Impact factor: 4.314

4.  Mirk protein kinase is a mitogen-activated protein kinase substrate that mediates survival of colon cancer cells.

Authors:  K Lee; X Deng; E Friedman
Journal:  Cancer Res       Date:  2000-07-01       Impact factor: 12.701

Review 5.  Mirk/Dyrk1B: a multifunctional dual-specificity kinase involved in growth arrest, differentiation, and cell survival.

Authors:  Stephen E Mercer; Eileen Friedman
Journal:  Cell Biochem Biophys       Date:  2006       Impact factor: 2.194

6.  Manipulation of alternative splicing by a newly developed inhibitor of Clks.

Authors:  Michiko Muraki; Bisei Ohkawara; Takamitsu Hosoya; Hiroshi Onogi; Jun Koizumi; Tomonobu Koizumi; Kengo Sumi; Jun-ichiro Yomoda; Michael V Murray; Hiroshi Kimura; Kiyoshi Furuichi; Hiroshi Shibuya; Adrian R Krainer; Masaaki Suzuki; Masatoshi Hagiwara
Journal:  J Biol Chem       Date:  2004-03-08       Impact factor: 5.157

7.  Sequence characteristics, subcellular localization, and substrate specificity of DYRK-related kinases, a novel family of dual specificity protein kinases.

Authors:  W Becker; Y Weber; K Wetzel; K Eirmbter; F J Tejedor; H G Joost
Journal:  J Biol Chem       Date:  1998-10-02       Impact factor: 5.157

8.  Mirk regulates the exit of colon cancer cells from quiescence.

Authors:  Kideok Jin; Daina Z Ewton; Sunju Park; Jing Hu; Eileen Friedman
Journal:  J Biol Chem       Date:  2009-06-19       Impact factor: 5.157

9.  Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.

Authors:  Oleg Fedorov; Kilian Huber; Andreas Eisenreich; Panagis Filippakopoulos; Oliver King; Alex N Bullock; Damian Szklarczyk; Lars J Jensen; Doriano Fabbro; Jörg Trappe; Ursula Rauch; Franz Bracher; Stefan Knapp
Journal:  Chem Biol       Date:  2011-01-28

10.  The protein kinase DYRK1A phosphorylates the splicing factor SF3b1/SAP155 at Thr434, a novel in vivo phosphorylation site.

Authors:  Katrin de Graaf; Hanna Czajkowska; Sabine Rottmann; Len C Packman; Richard Lilischkis; Bernhard Lüscher; Walter Becker
Journal:  BMC Biochem       Date:  2006-03-02       Impact factor: 4.059
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  26 in total

1.  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

2.  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

3.  The Tumor Suppressor NKX3.1 Is Targeted for Degradation by DYRK1B Kinase.

Authors:  Liang-Nian Song; Jose Silva; Antonius Koller; Andrew Rosenthal; Emily I Chen; Edward P Gelmann
Journal:  Mol Cancer Res       Date:  2015-03-16       Impact factor: 5.852

4.  Novel and Potential Small Molecule Scaffolds as DYRK1A Inhibitors by Integrated Molecular Docking-Based Virtual Screening and Dynamics Simulation Study.

Authors:  Mir Mohammad Shahroz; Hemant Kumar Sharma; Abdulmalik S A Altamimi; Mubarak A Alamri; Abuzer Ali; Amena Ali; Safar Alqahtani; Ali Altharawi; Alhumaidi B Alabbas; Manal A Alossaimi; Yassine Riadi; Ahmad Firoz; Obaid Afzal
Journal:  Molecules       Date:  2022-02-09       Impact factor: 4.411

Review 5.  Current pharmacotherapy and putative disease-modifying therapy for Alzheimer's disease.

Authors:  Akanksha Kulshreshtha; Poonam Piplani
Journal:  Neurol Sci       Date:  2016-06-01       Impact factor: 3.307

Review 6.  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

7.  Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.

Authors:  Thomas C Coombs; Cordelle Tanega; Min Shen; Jenna L Wang; Douglas S Auld; Samuel W Gerritz; Frank J Schoenen; Craig J Thomas; Jeffrey Aubé
Journal:  Bioorg Med Chem Lett       Date:  2013-03-30       Impact factor: 2.823

8.  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

9.  Pharmacophore and 3D-QSAR characterization of 6-arylquinazolin-4-amines as Cdc2-like kinase 4 (Clk4) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (Dyrk1A) inhibitors.

Authors:  Yongmei Pan; Yanli Wang; Stephen H Bryant
Journal:  J Chem Inf Model       Date:  2013-04-04       Impact factor: 4.956

10.  Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.

Authors:  Vassilios Myrianthopoulos; Marina Kritsanida; Nicolas Gaboriaud-Kolar; Prokopios Magiatis; Yoan Ferandin; Emilie Durieu; Olivier Lozach; Daniel Cappel; Meera Soundararajan; Panagis Filippakopoulos; Woody Sherman; Stefan Knapp; Laurent Meijer; Emmanuel Mikros; Alexios-Leandros Skaltsounis
Journal:  ACS Med Chem Lett       Date:  2012-11-01       Impact factor: 4.345
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