Search Results - "Holskin, Beverly"
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Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells
Published in Blood (15-02-2006)“…The roles of aberrant expression of constitutively active ALK chimeric proteins in the pathogenesis of anaplastic large-cell lymphoma (ALCL) have been well…”
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ALK Mutants in the Kinase Domain Exhibit Altered Kinase Activity and Differential Sensitivity to Small Molecule ALK Inhibitors
Published in Biochemistry (Easton) (28-04-2009)“…Abnormal expression of constitutively active anaplastic lymphoma kinase (ALK) chimeric proteins in the pathogenesis of anaplastic large-cell lymphoma (ALCL) is…”
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Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models
Published in Journal of medicinal chemistry (25-09-2008)“…The optimization of the dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-one R2 and R12 positions led to the identification of the first MLK1 and MLK3…”
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Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: Identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test
Published in Bioorganic & medicinal chemistry letters (01-02-2012)“…Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine6 (5-HT6) receptor…”
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Improvement of inhibitor identification for heat shock protein 90α by utilizing a red-shifted fluorescence polarization probe
Published in Assay and drug development technologies (01-08-2012)“…Heat shock protein-90 (HSP90) is an ATP-dependent molecular chaperone with intrinsic ATPase activity. HSP90 is required for the stability and function of…”
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Comparison of two homogeneous cell-based kinase assays for JAK2 V617F: SureFire pSTAT5 and GeneBLAzer fluorescence resonance energy transfer assays
Published in Assay and drug development technologies (01-04-2012)“…The Janus kinase (JAK)/signal transducer and activator of transcription (STAT) signaling pathway plays an important role in cellular responses to cytokines and…”
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Modification of CellSensor irf1-bla TF-1 and irf1-bla HEL assays for direct comparison of wild-type JAK2 and JAK2 V617F inhibition
Published in Assay and drug development technologies (01-06-2011)“…The Janus kinase (JAK)-signal transducer and activator of transcription pathway is an important therapeutic target because of its role in the regulation of…”
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Inhibition of mixed lineage kinase 3 attenuates MPP +-induced neurotoxicity in SH-SY5Y cells
Published in Brain research (02-04-2004)“…The neuropathology of Parkinson's Disease has been modeled in experimental animals following MPTP treatment and in dopaminergic cells in culture treated with…”
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Phosphoregulation of Mixed-Lineage Kinase 1 Activity by Multiple Phosphorylation in the Activation Loop
Published in Biochemistry (Easton) (28-12-2004)“…Mixed-lineage kinase 1 (MLK1) is a mitogen-activated protein kinase kinase kinase capable of activating the c-Jun NH2-terminal kinase (JNK) pathway…”
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Aequorin functional assay for characterization of G-protein-coupled receptors: Implementation with cryopreserved transiently transfected cells
Published in Analytical biochemistry (15-05-2010)“…Assay technologies that measure intracellular Ca 2+ release are among the predominant methods for evaluation of GPCR function. These measurements have…”
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Comparison of two homogeneous cell‐based kinase assays for JAK2 V617F: SureFire™ pSTAT5 and GeneBLAzer® FRET assays
Published in The FASEB journal (01-04-2009)“…Abstract only The Janus kinase (JAK)/Signal Transducers and Activators of Transcription (STAT) signaling pathway plays an important role in cellular responses…”
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Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-01-2012)“…h5-HT6R Ki=4.4nM; h5-HT6R cAMP IC50=9.8nM; estimated rat % F=36; brain/plasma: 2. 7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel…”
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Induction by E1A oncogene expression of cellular susceptibility to lysis by TNF
Published in Nature (London) (10-12-1987)“…Tumour necrosis factor alpha (ref. 1), synthesized primarily by monocytes in response to various invasive agents, induces a wide variety of biological effects…”
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