Published in Biochem J on March 15, 2010
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Small molecule inhibitors of aurora-a induce proteasomal degradation of N-myc in childhood neuroblastoma. Cancer Cell (2013) 1.85
Aurora A kinase (AURKA) in normal and pathological cell division. Cell Mol Life Sci (2012) 1.84
Drugging MYCN through an allosteric transition in Aurora kinase A. Cancer Cell (2014) 1.33
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Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors. J Med Chem (2012) 1.09
On the molecular mechanisms of mitotic kinase activation. Open Biol (2012) 1.08
Pten regulates Aurora-A and cooperates with Fbxw7 in modulating radiation-induced tumor development. Mol Cancer Res (2012) 1.05
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Structural basis of N-Myc binding by Aurora-A and its destabilization by kinase inhibitors. Proc Natl Acad Sci U S A (2016) 0.86
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Basal aurora kinase B activity is sufficient for histone H3 phosphorylation in prophase. Biol Open (2013) 0.82
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Diverse functionalization of Aurora-A kinase at specified surface and buried sites by native chemical modification. PLoS One (2014) 0.79
Tripolin A, a novel small-molecule inhibitor of aurora A kinase, reveals new regulation of HURP's distribution on microtubules. PLoS One (2013) 0.78
Conformational analysis of the DFG-out kinase motif and biochemical profiling of structurally validated type II inhibitors. J Med Chem (2014) 0.78
Structure of Aurora B-INCENP in complex with barasertib reveals a potential transinhibitory mechanism. Acta Crystallogr F Struct Biol Commun (2014) 0.77
Identifying three-dimensional structures of autophosphorylation complexes in crystals of protein kinases. Sci Signal (2015) 0.77
Specificity rendering 'hot-spots' for aurora kinase inhibitor design: the role of non-covalent interactions and conformational transitions. PLoS One (2014) 0.76
A water-mediated allosteric network governs activation of Aurora kinase A. Nat Chem Biol (2017) 0.75
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Dynamic Equilibrium of the Aurora-A Kinase Activation Loop Revealed by Single Molecule Spectroscopy. Angew Chem Int Ed Engl (2017) 0.75
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A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. Cancer Res (2010) 2.05
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem (2010) 2.04
A public-private partnership to unlock the untargeted kinome. Nat Chem Biol (2013) 1.83
Cell cycle regulation by the NEK family of protein kinases. J Cell Sci (2012) 1.64
Structures of two core subunits of the bacterial type IV secretion system, VirB8 from Brucella suis and ComB10 from Helicobacter pylori. Proc Natl Acad Sci U S A (2005) 1.39
Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation. J Clin Endocrinol Metab (2004) 1.36
A large domain swap in the VirB11 ATPase of Brucella suis leaves the hexameric assembly intact. J Mol Biol (2006) 1.26
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Agrobacterium VirB10 domain requirements for type IV secretion and T pilus biogenesis. Mol Microbiol (2008) 1.21
Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity. Mol Cancer Ther (2005) 1.15
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An autoinhibitory tyrosine motif in the cell-cycle-regulated Nek7 kinase is released through binding of Nek9. Mol Cell (2009) 1.12
Scaffold diversity of exemplified medicinal chemistry space. J Chem Inf Model (2011) 1.11
Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol Cancer Ther (2007) 1.08
Insights into the conformational variability and regulation of human Nek2 kinase. J Mol Biol (2008) 1.07
Coordination of adjacent domains mediates TACC3-ch-TOG-clathrin assembly and mitotic spindle binding. J Cell Biol (2013) 1.06
Functional Tat transport of unstructured, small, hydrophilic proteins. J Biol Chem (2007) 1.06
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The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Mol Cancer Ther (2011) 1.05
Crystal structures of the phosphorylated BRI1 kinase domain and implications for brassinosteroid signal initiation. Plant J (2014) 1.03
Structural basis of poly(ADP-ribose) recognition by the multizinc binding domain of checkpoint with forkhead-associated and RING Domains (CHFR). J Biol Chem (2010) 0.99
The Nek8 protein kinase, mutated in the human cystic kidney disease nephronophthisis, is both activated and degraded during ciliogenesis. Hum Mol Genet (2011) 0.99
Dimerization and interactions of Brucella suis VirB8 with VirB4 and VirB10 are required for its biological activity. Proc Natl Acad Sci U S A (2006) 0.98
Evaluation of germline BMP4 mutation as a cause of colorectal cancer. Hum Mutat (2010) 0.98
Crystal structure of EML1 reveals the basis for Hsp90 dependence of oncogenic EML4-ALK by disruption of an atypical β-propeller domain. Proc Natl Acad Sci U S A (2014) 0.98
The importance of occupancy rather than affinity of CaV(beta) subunits for the calcium channel I-II linker in relation to calcium channel function. J Physiol (2006) 0.97
Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization. J Med Chem (2010) 0.97
Insights into Aurora-A kinase activation using unnatural amino acids incorporated by chemical modification. ACS Chem Biol (2013) 0.97
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem (2013) 0.96
A cancer-associated aurora A mutant is mislocalized and misregulated due to loss of interaction with TPX2. J Biol Chem (2009) 0.95
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship. J Med Chem (2011) 0.94
A kinetic test characterizes kinase intramolecular and intermolecular autophosphorylation mechanisms. Sci Signal (2013) 0.93
Selective delivery of CB300638, a cyclopenta[g]quinazoline-based thymidylate synthase inhibitor into human tumor cell lines overexpressing the alpha-isoform of the folate receptor. Cancer Res (2003) 0.92
Identification, structure and mode of action of a new regulator of the Helicobacter pylori HP0525 ATPase. EMBO J (2007) 0.91
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells. Bioorg Med Chem Lett (2010) 0.90
Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. J Med Chem (2007) 0.90
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Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. J Med Chem (2012) 0.88
The metabolism and toxicity of furosemide in the Wistar rat and CD-1 mouse: a chemical and biochemical definition of the toxicophore. J Pharmacol Exp Ther (2007) 0.88
Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells. J Med Chem (2013) 0.88
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase. J Med Chem (2007) 0.87
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Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs). Bioorg Med Chem (2008) 0.85
Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B. Bioorg Med Chem (2005) 0.84
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Targeting the alpha-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase. Bioorg Med Chem (2006) 0.82
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Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Bioorg Med Chem Lett (2010) 0.81
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. Bioorg Med Chem Lett (2008) 0.80
The tetrahydrobiopterin pathway and pain. Curr Opin Investig Drugs (2010) 0.80
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Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today (2007) 0.79
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. J Med Chem (2010) 0.79
The structural mechanisms that underpin mitotic kinase activation. Biochem Soc Trans (2013) 0.79
A pocket on the surface of the N-terminal BRCT domain of Mcph1 is required to prevent abnormal chromosome condensation. J Mol Biol (2009) 0.78
Epigenetics: Targeting leukemia on the DOT. Nat Chem Biol (2011) 0.78
Repeatability of a dental shade-matching instrument when compared to traditional visual methods of shade evaluation. Gen Dent (2009) 0.77
Benzimidazole inhibitors of the protein kinase CHK2: clarification of the binding mode by flexible side chain docking and protein-ligand crystallography. Bioorg Med Chem (2012) 0.77
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors. Bioorg Med Chem (2011) 0.77
Design and synthesis of pyridazinone-based 5-HT(2C) agonists. Bioorg Med Chem Lett (2009) 0.76
Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2. PLoS One (2013) 0.75
Measurement of clinicians' ability to hand torque dental implant components. J Oral Implantol (2009) 0.75
Resonance assignments of the complex between TraN and the C-terminal domain of TraO from the conjugative plasmid pKM101. J Biomol NMR (2006) 0.75
ClTi(OiPr)3-promoted reductive amination on the solid phase: combinatorial synthesis of a biaryl-based sulfonamide library. J Comb Chem (2008) 0.75
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists. Bioorg Med Chem Lett (2009) 0.75
Erratum: The structure of Legionella pneumophila LegK4 type four secretion system (T4SS) effector reveals a novel dimeric eukaryotic-like kinase. Sci Rep (2016) 0.75
Regioselective C2-arylation of imidazo[4,5-b]pyridines. Org Biomol Chem (2013) 0.75
Characterization of three druggable hotspots in the Aurora-A/TPX2 interaction using biochemical, biophysical and fragment-based approaches. ACS Chem Biol (2017) 0.75
Analysis of water patterns in protein kinase binding sites. Proteins (2011) 0.75
The arrogance of youth. Lancet (2004) 0.75
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