Published in Bioorg Med Chem Lett on March 30, 2013
Identification of a novel function of CX-4945 as a splicing regulator. PLoS One (2014) 0.89
Inhibition of DYRK1A Stimulates Human β-Cell Proliferation. Diabetes (2016) 0.86
DYRK1A, a Dosage-Sensitive Gene Involved in Neurodevelopmental Disorders, Is a Target for Drug Development in Down Syndrome. Front Behav Neurosci (2016) 0.79
The Tumor Suppressor NKX3.1 Is Targeted for Degradation by DYRK1B Kinase. Mol Cancer Res (2015) 0.76
Pharmacology of Modulators of Alternative Splicing. Pharmacol Rev (2017) 0.75
Synthesis and SAR studies of novel 6,7,8-substituted 4-substituted benzyloxyquinolin-2(1H)-one derivatives for anticancer activity. Br J Pharmacol (2015) 0.75
The SR protein family of splicing factors: master regulators of gene expression. Biochem J (2009) 5.98
Alternative splicing in disease and therapy. Nat Biotechnol (2004) 4.85
Dyrk1A haploinsufficiency affects viability and causes developmental delay and abnormal brain morphology in mice. Mol Cell Biol (2002) 2.51
Sequence characteristics, subcellular localization, and substrate specificity of DYRK-related kinases, a novel family of dual specificity protein kinases. J Biol Chem (1998) 2.29
Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem (2004) 2.26
Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol (2011) 2.06
Cdc2-like kinase 2 is an insulin-regulated suppressor of hepatic gluconeogenesis. Cell Metab (2010) 1.75
Truncation of the Down syndrome candidate gene DYRK1A in two unrelated patients with microcephaly. Am J Hum Genet (2008) 1.70
DYRK1A and DYRK3 promote cell survival through phosphorylation and activation of SIRT1. J Biol Chem (2010) 1.65
The Clk2 and Clk3 dual-specificity protein kinases regulate the intranuclear distribution of SR proteins and influence pre-mRNA splicing. Exp Cell Res (1998) 1.63
DYRK family of protein kinases: evolutionary relationships, biochemical properties, and functional roles. FASEB J (2010) 1.55
Human minibrain homologue (MNBH/DYRK1): characterization, alternative splicing, differential tissue expression, and overexpression in Down syndrome. Genomics (1999) 1.55
DYRK1B-dependent autocrine-to-paracrine shift of Hedgehog signaling by mutant RAS. Nat Struct Mol Biol (2010) 1.49
Characterization and comparison of four serine- and arginine-rich (SR) protein kinases. Biochem J (1997) 1.49
Function and regulation of Dyrk1A: towards understanding Down syndrome. Cell Mol Life Sci (2009) 1.44
Dyrk1A overexpression inhibits proliferation and induces premature neuronal differentiation of neural progenitor cells. J Neurosci (2010) 1.37
MNB/DYRK1A as a multiple regulator of neuronal development. FEBS J (2010) 1.36
Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation. Structure (2009) 1.36
Alternative splicing: a new drug target of the post-genome era. Biochim Biophys Acta (2005) 1.30
Harmine specifically inhibits protein kinase DYRK1A and interferes with neurite formation. FEBS J (2009) 1.29
Utilization of operational schemes for analog synthesis in drug design. J Med Chem (1972) 1.26
Mirk/Dyrk1B in cancer. J Cell Biochem (2007) 1.25
Akt2 regulation of Cdc2-like kinases (Clk/Sty), serine/arginine-rich (SR) protein phosphorylation, and insulin-induced alternative splicing of PKCbetaII messenger ribonucleic acid. Endocrinology (2008) 1.24
The role of DYRK1A in neurodegenerative diseases. FEBS J (2010) 1.23
Regulation and substrate specificity of the SR protein kinase Clk/Sty. Mol Cell Biol (2003) 1.20
Activation, regulation, and inhibition of DYRK1A. FEBS J (2010) 1.18
Mirk/Dyrk1B: a multifunctional dual-specificity kinase involved in growth arrest, differentiation, and cell survival. Cell Biochem Biophys (2006) 1.17
Constitutive Dyrk1A is abnormally expressed in Alzheimer disease, Down syndrome, Pick disease, and related transgenic models. Neurobiol Dis (2005) 1.16
The dual-specificity CLK kinase induces neuronal differentiation of PC12 cells. Mol Cell Biol (1994) 1.15
Role for DYRK family kinases on regulation of apoptosis. Biochem Pharmacol (2008) 1.14
The protein kinase DYRK1A phosphorylates the splicing factor SF3b1/SAP155 at Thr434, a novel in vivo phosphorylation site. BMC Biochem (2006) 1.10
Cloning and characterization of DYRK1B, a novel member of the DYRK family of protein kinases. Biochem Biophys Res Commun (1999) 1.10
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk). Bioorg Med Chem Lett (2009) 1.06
Comparison of bioluminescent kinase assays using substrate depletion and product formation. Assay Drug Dev Technol (2009) 1.04
Combination of Clk family kinase and SRp75 modulates alternative splicing of Adenovirus E1A. Genes Cells (2008) 1.01
Cdc2-like kinases and DNA topoisomerase I regulate alternative splicing of tissue factor in human endothelial cells. Circ Res (2009) 1.01
Harmine is an ATP-competitive inhibitor for dual-specificity tyrosine phosphorylation-regulated kinase 1A (Dyrk1A). Arch Biochem Biophys (2010) 1.00
Differential effect of CLK SR Kinases on HIV-1 gene expression: potential novel targets for therapy. Retrovirology (2011) 0.99
Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). Bioorg Med Chem Lett (2011) 0.89
The dual specificity protein kinase CLK3 is abundantly expressed in mature mouse spermatozoa. Exp Cell Res (1999) 0.84
Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries. Proc Natl Acad Sci U S A (2006) 9.92
Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature (2010) 8.78
Genomewide association study of leprosy. N Engl J Med (2009) 8.17
Genome-wide association study in a Chinese Han population identifies nine new susceptibility loci for systemic lupus erythematosus. Nat Genet (2009) 6.42
Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses. Science (2011) 5.72
High-throughput screening assays for the identification of chemical probes. Nat Chem Biol (2007) 4.50
Hematotoxicity in workers exposed to low levels of benzene. Science (2004) 4.19
Noncanonical TGFβ signaling contributes to aortic aneurysm progression in Marfan syndrome mice. Science (2011) 3.49
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol (2012) 3.40
Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways. Proc Natl Acad Sci U S A (2011) 3.20
Identification of oxadiazoles as new drug leads for the control of schistosomiasis. Nat Med (2008) 2.90
Shortened telomere length is associated with increased risk of cancer: a meta-analysis. PLoS One (2011) 2.61
Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). J Immunol (2011) 2.59
Fluorescence spectroscopic profiling of compound libraries. J Med Chem (2008) 2.53
High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells. Proc Natl Acad Sci U S A (2014) 2.50
A prospective study of telomere length measured by monochrome multiplex quantitative PCR and risk of non-Hodgkin lymphoma. Clin Cancer Res (2009) 2.48
COPI complex is a regulator of lipid homeostasis. PLoS Biol (2008) 2.47
Cooperative epigenetic modulation by cancer amplicon genes. Cancer Cell (2010) 2.43
Occupational exposure to formaldehyde, hematotoxicity, and leukemia-specific chromosome changes in cultured myeloid progenitor cells. Cancer Epidemiol Biomarkers Prev (2010) 2.34
Isolation and characterization of tumorigenic extrahepatic cholangiocarcinoma cells with stem cell-like properties. Int J Cancer (2011) 2.12
Cytokine polymorphisms in the Th1/Th2 pathway and susceptibility to non-Hodgkin lymphoma. Blood (2006) 2.06
A low-molecular-weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism. Endocrinology (2008) 2.03
Rational selection of training and test sets for the development of validated QSAR models. J Comput Aided Mol Des (2003) 2.01
Segmental hair analysis after a single dose of zolpidem: comparison with a previous study. J Anal Toxicol (2013) 1.98
Analysis of 50 SNPs in CYP2D6, CYP2C19, CYP2C9, CYP3A4 and CYP1A2 by MALDI-TOF mass spectrometry in Chinese Han population. Forensic Sci Int (2010) 1.96
A genome-wide association study identifies two new risk loci for Graves' disease. Nat Genet (2011) 1.92
The 5p15.33 locus is associated with risk of lung adenocarcinoma in never-smoking females in Asia. PLoS Genet (2010) 1.90
Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology. Chem Biol (2010) 1.83
Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants. Biochemistry (2008) 1.82
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase. J Med Chem (2008) 1.81
CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP. Blood (2010) 1.77
Apparent activity in high-throughput screening: origins of compound-dependent assay interference. Curr Opin Chem Biol (2010) 1.76
Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns. J Med Chem (2006) 1.71
Genome-wide association study for vitiligo identifies susceptibility loci at 6q27 and the MHC. Nat Genet (2010) 1.69
Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124. Proc Natl Acad Sci U S A (2010) 1.64
Serum cotinine level as predictor of lung cancer risk. Cancer Epidemiol Biomarkers Prev (2006) 1.63
Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Proc Natl Acad Sci U S A (2009) 1.61
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem (2010) 1.61
Enhancing antibody Fc heterodimer formation through electrostatic steering effects: applications to bispecific molecules and monovalent IgG. J Biol Chem (2010) 1.60
Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade. PLoS Negl Trop Dis (2008) 1.58
Mitochondrial DNA copy number and lung cancer risk in a prospective cohort study. Carcinogenesis (2010) 1.56
Oxidative damage-related genes AKR1C3 and OGG1 modulate risks for lung cancer due to exposure to PAH-rich coal combustion emissions. Carcinogenesis (2004) 1.47
Variation in lung cancer risk by smoky coal subtype in Xuanwei, China. Int J Cancer (2008) 1.45
Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. J Med Chem (2010) 1.45
A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR). J Biol Chem (2006) 1.38
Using urinary biomarkers to elucidate dose-related patterns of human benzene metabolism. Carcinogenesis (2005) 1.37
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett (2010) 1.37
Facile C-N cleavage in a series of bridged lactams. J Am Chem Soc (2005) 1.37
A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution. J Med Chem (2009) 1.34
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series. Bioorg Med Chem Lett (2007) 1.32
Genetic variants in caspase genes and susceptibility to non-Hodgkin lymphoma. Carcinogenesis (2006) 1.32
Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1. PLoS One (2009) 1.32
Pathway-based evaluation of 380 candidate genes and lung cancer susceptibility suggests the importance of the cell cycle pathway. Carcinogenesis (2008) 1.32
Revisiting a classic approach to the Aspidosperma alkaloids: an intramolecular Schmidt reaction mediated synthesis of (+)-aspidospermidine. J Org Chem (2005) 1.31
Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries. Nat Biotechnol (2009) 1.30
Tuning the optical properties of fluorinated indolylfulgimides. J Org Chem (2003) 1.29
Interleukin-36 (IL-36) ligands require processing for full agonist (IL-36α, IL-36β, and IL-36γ) or antagonist (IL-36Ra) activity. J Biol Chem (2011) 1.28
Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening. Biochemistry (2009) 1.28
Luteolin limits infarct size and improves cardiac function after myocardium ischemia/reperfusion injury in diabetic rats. PLoS One (2012) 1.27
Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays. PLoS One (2013) 1.27
Modeling human metabolism of benzene following occupational and environmental exposures. Cancer Epidemiol Biomarkers Prev (2006) 1.26
Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition. J Med Chem (2007) 1.26
Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor. J Biomol Screen (2008) 1.25
Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem (2013) 1.25
Characterization of a Cdc42 protein inhibitor and its use as a molecular probe. J Biol Chem (2013) 1.24
Discovery of novel biomarkers by microarray analysis of peripheral blood mononuclear cell gene expression in benzene-exposed workers. Environ Health Perspect (2005) 1.24
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H. J Med Chem (2011) 1.24
Genetic polymorphisms in the oxidative stress pathway and susceptibility to non-Hodgkin lymphoma. Hum Genet (2006) 1.24
The opposite-direction modulation of CD4+CD25+ Tregs and T helper 1 cells in acute coronary syndromes. Clin Immunol (2007) 1.22
A dual-fluorescence high-throughput cell line system for probing multidrug resistance. Assay Drug Dev Technol (2009) 1.22
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem (2005) 1.21
A virtual screen for diverse ligands: discovery of selective G protein-coupled receptor antagonists. J Am Chem Soc (2008) 1.20
Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening. Assay Drug Dev Technol (2009) 1.20
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. Endocrinology (2010) 1.20
Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008. J Comb Chem (2009) 1.19
Auranofin induces lethal oxidative and endoplasmic reticulum stress and exerts potent preclinical activity against chronic lymphocytic leukemia. Cancer Res (2014) 1.19
A genome-wide association study in Han Chinese identifies a susceptibility locus for primary Sjögren's syndrome at 7q11.23. Nat Genet (2013) 1.19
Cation-pi control of regiochemistry of intramolecular schmidt reactions en route to bridged bicyclic lactams. J Am Chem Soc (2007) 1.18
Development of functionally selective, small molecule agonists at kappa opioid receptors. J Biol Chem (2013) 1.17
Polymorphisms in cytokine and cellular adhesion molecule genes and susceptibility to hematotoxicity among workers exposed to benzene. Cancer Res (2005) 1.16
A novel small molecule inhibitor of hepatitis C virus entry. PLoS Pathog (2010) 1.16
Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter. Chem Biol (2012) 1.14
A combined intramolecular Diels-Alder/intramolecular schmidt reaction: formal synthesis of (+/-)-stenine. Angew Chem Int Ed Engl (2002) 1.14
Domino reactions that combine an azido-Schmidt ring expansion with the Diels-Alder reaction. Org Lett (2004) 1.14
Identification of clinically used drugs that activate pregnane X receptors. Drug Metab Dispos (2010) 1.14
Mechanistic studies with potent and selective inducible nitric-oxide synthase dimerization inhibitors. J Biol Chem (2001) 1.14
TCR signaling via Tec kinase ITK and interferon regulatory factor 4 (IRF4) regulates CD8+ T-cell differentiation. Proc Natl Acad Sci U S A (2012) 1.13
Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion. Proc Natl Acad Sci U S A (2010) 1.13