Synthesis and evaluation of new potent inhibitors of CK1 and CDK5, two kinases involved in Alzheimer’s disease

[1]  A. Katritzky,et al.  Heterocycles , 2022, Pharmaceutical Chemistry Journal.

[2]  H. Bregman,et al.  Structure-Based Design of Potent and Selective CK1γ Inhibitors. , 2012, ACS medicinal chemistry letters.

[3]  A. Ittner,et al.  Tau‐targeted treatment strategies in Alzheimer's disease , 2012, British journal of pharmacology.

[4]  L. Meijer,et al.  Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues: a novel DYRK1A inhibitor class. , 2012, European journal of medicinal chemistry.

[5]  U. Knippschild,et al.  2-Benzamido-N-(1H-benzo[d]imidazol-2-yl)thiazole-4-carboxamide derivatives as potent inhibitors of CK1δ/ε , 2012, Amino Acids.

[6]  R. Vassar,et al.  Cdk5 Protein Inhibition and Aβ42 Increase BACE1 Protein Level in Primary Neurons by a Post-transcriptional Mechanism , 2012, The Journal of Biological Chemistry.

[7]  Miguel Medina,et al.  Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3β by Tideglusib* , 2011, The Journal of Biological Chemistry.

[8]  Arup K. Ghose,et al.  Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery , 2011, ACS chemical neuroscience.

[9]  Carmen Gil,et al.  Protein kinases CK1 and CK2 as new targets for neurodegenerative diseases , 2011, Medicinal research reviews.

[10]  F. Terro,et al.  Tau phosphorylation and neuronal apoptosis induced by the blockade of PP2A preferentially involve GSK3β , 2011, Neurochemistry International.

[11]  L. Gravitz.  Drugs: A tangled web of targets , 2011, Nature.

[12]  L. Meijer,et al.  Synthesis, protein kinase inhibitory potencies, and in vitro antiproliferative activities of meridianin derivatives. , 2011, Journal of medicinal chemistry.

[13]  V. Kanase,et al.  Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity. , 2011, European journal of medicinal chemistry.

[14]  L. Meijer,et al.  Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. , 2011, Journal of medicinal chemistry.

[15]  T. Misteli,et al.  Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). , 2011, Bioorganic & medicinal chemistry letters.

[16]  T. Dunckley,et al.  β-Carboline Compounds, Including Harmine, Inhibit DYRK1A and Tau Phosphorylation at Multiple Alzheimer's Disease-Related Sites , 2011, PloS one.

[17]  K. Kosik,et al.  Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors. , 2011, Bioorganic & medicinal chemistry letters.

[18]  Jürgen Götz,et al.  Amyloid-β and tau — a toxic pas de deux in Alzheimer's disease , 2011, Nature Reviews Neuroscience.

[19]  Ezzie Hutchinson,et al.  Systems neuroscience: The stress of dieting , 2011, Nature Reviews Neuroscience.

[20]  J. Wegiel,et al.  The role of DYRK1A in neurodegenerative diseases , 2011, The FEBS journal.

[21]  W. Sippl,et al.  Activation, regulation, and inhibition of DYRK1A , 2011, The FEBS journal.

[22]  J. Snyder,et al.  A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. , 2010, Journal of medicinal chemistry.

[23]  M. Beller,et al.  Synthesis of Novel Annulated Hymenialdisine Analogues via Palladium-Catalyzed Cross-Coupling Reactions with Aryl Boronic Acids. , 2010 .

[24]  C. Kenific,et al.  Purine derivatives as potent gamma-secretase modulators. , 2010, Bioorganic & medicinal chemistry letters.

[25]  Mohammed M. Abadleh,et al.  3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta. , 2009, Journal of medicinal chemistry.

[26]  Philippe Bernard,et al.  Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue. , 2009, Journal of medicinal chemistry.

[27]  P. Greengard,et al.  Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. , 2008, Journal of medicinal chemistry.

[28]  J. Wegiel,et al.  The role of overexpressed DYRK1A protein in the early onset of neurofibrillary degeneration in Down syndrome , 2008, Acta Neuropathologica.

[29]  L. Meijer,et al.  Synthesis of 6-Pyridylaminopurines , 2008 .

[30]  L Meijer,et al.  CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases , 2008, Oncogene.

[31]  L. Meijer,et al.  Purification of CK1 by affinity chromatography on immobilised axin. , 2007, Protein expression and purification.

[32]  P. Greengard,et al.  Regulation of Alzheimer's disease amyloid-β formation by casein kinase I , 2007, Proceedings of the National Academy of Sciences.

[33]  P. S. Klein,et al.  Multiple roles for glycogen synthase kinase-3 as a drug target in Alzheimer's disease. , 2006, Current drug targets.

[34]  L. Meijer,et al.  (R)-Roscovitine (CYC202, Seliciclib) , 2006 .

[35]  L. Tsai,et al.  p25/Cyclin-Dependent Kinase 5 Induces Production and Intraneuronal Accumulation of Amyloid β In Vivo , 2006, The Journal of Neuroscience.

[36]  M. Pallàs,et al.  The role of CDK5/P25 formation/inhibition in neurodegeneration. , 2006, Drug news & perspectives.

[37]  D. Grierson,et al.  The purines: potent and versatile small molecule inhibitors and modulators of key biological targets. , 2006, Bioorganic & medicinal chemistry.

[38]  D. Borghi,et al.  A new glycociamidine ring precursor: syntheses of (Z)-hymenialdisine, (Z)-2-debromohymenialdisine, and (+/-)-endo-2-debromohymenialdisine. , 2005, Organic letters.

[39]  Lin Tang,et al.  Roscovitine Targets, Protein Kinases and Pyridoxal Kinase*[boxs] , 2005, Journal of Biological Chemistry.

[40]  Li-Huei Tsai,et al.  Cdk5 deregulation in the pathogenesis of Alzheimer's disease. , 2004, Trends in molecular medicine.

[41]  L. Meijer,et al.  Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling. , 2013, Bioorganic & medicinal chemistry letters.

[42]  Fei Wang,et al.  Discovery of potent small molecule inhibitors of DYRK1A by structure-based virtual screening and bioassay. , 2012, Bioorganic & medicinal chemistry letters.

[43]  M. Beller,et al.  Synthesis of Novel AnnulatedHymenialdisine Analogues via Palladium-Catalyzed Cross-CouplingReactions with Aryl Boronic Acids , 2010 .

[44]  P. Greengard,et al.  Regulation of Alzheimer's disease amyloid-beta formation by casein kinase I. , 2007, Proceedings of the National Academy of Sciences of the United States of America.

[45]  L Meijer,et al.  Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent. , 2000, Chemistry & biology.