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Genomes and Genes | Georg C TerstappenSummaryAffiliation: Discovery Research Country: Italy Publications
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Publications
Target deconvolution strategies in drug discoveryGeorg C Terstappen
Siena Biotech S p A, Via Fiorentina 1, 53100 Siena, Italy
Nat Rev Drug Discov 6:891-903. 2007..Here, the broad panel of experimental strategies that can be applied to target deconvolution is critically reviewed...- Drug discovery and development for Huntington's disease - an orphan indication with high medical needFreddy Heitz
Siena Biotech SpA, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy
IDrugs 11:653-60. 2008..Thus, hope exists for patients with HD that efficacious medicines will become available... - Detection of phosphorylation patterns in rat cortical neurons by combining phosphatase treatment and DIGE technologyRoberto Raggiaschi
Discovery Research, Sienabiotech S p A, Siena, Italy
Proteomics 6:748-56. 2006..The analysis of 42 selected spots was carried out by LC/MS/MS technology resulting in the identification of two new phosphoproteins... - The Wnt signaling pathway as a target for the treatment of neurodegenerative disordersGeorg C Terstappen
Sienabiotech SpA, Via Fiorentina 1, 53100 Siena, Italy
IDrugs 9:35-8. 2006..With the recent accumulation of evidence that the Wnt signaling pathway might be impaired in such diseases, a new avenue for potential therapeutic intervention has been opened which comprises many putative drug targets... - Inhibition of Wnt signaling, modulation of Tau phosphorylation and induction of neuronal cell death by DKK1Carla Scali
Siena Biotech S p A, 53100 Siena, Italy
Neurobiol Dis 24:254-65. 2006..The demonstration that DKK1 inhibits Wnt signaling in neurons and causes neuronal death supports the hypothesis that inhibition of the canonical Wnt pathway contributes to the pathophysiology of neurodegenerative disorders... - Screening technologies for ion channel drug discoveryGeorg C Terstappen
Siena Biotech S p A, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy
Future Med Chem 2:715-30. 2010..In this review we provide an overview of the current repertoire of screening technologies that has evolved to drive ion channel-targeted drug discovery towards new medicines of the future... - The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3Georg C Terstappen
GlaxoSmithKline, Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy
Neurosci Lett 346:85-8. 2003..These results provide new information concerning the mechanism of therapeutic and/or side effects of one of the most widely used antidepressant drugs... - Nonradioactive rubidium ion efflux assay and its applications in drug discovery and developmentGeorg C Terstappen
Sienabiotech S p A, Discovery Research, Via Fiorentina 1, 53100 Siena, Italy
Assay Drug Dev Technol 2:553-9. 2004.... - Molecular cloning and characterization of a novel human variant of RIC-3, a putative chaperone of nicotinic acetylcholine receptorsTamara Seredenina
Siena Biotech S p A, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy
Biosci Rep 28:299-306. 2008..The RIC-3e protein is functionally active and enables surface expression of mature alpha7-nAChRs in cell lines not otherwise permissive for the expression of this receptor... - Procognitive and neuroprotective activity of a novel alpha7 nicotinic acetylcholine receptor agonist for treatment of neurodegenerative and cognitive disordersRenza Roncarati
Siena Biotech SpA, Siena, Italy
J Pharmacol Exp Ther 329:459-68. 2009.... - Functional properties of alpha7 nicotinic acetylcholine receptors co-expressed with RIC-3 in a stable recombinant CHO-K1 cell lineRenza Roncarati
Discovery Research, Siena Biotech S p A, Siena, Italy
Assay Drug Dev Technol 6:181-93. 2008..This recombinant cell system is useful for characterization of alpha7 nAChRs and to study the mechanism of action of chemical modulators, in particular the detection of PAMs capable of slowing receptor desensitization kinetics... - Increased expression of the oligopeptidase THOP1 is a neuroprotective response to Abeta toxicityGiuseppe Pollio
Siena Biotech SpA, Discovery Research, Via Fiorentina 1, 53100 Siena, Italy
Neurobiol Dis 31:145-58. 2008.... - Small molecule drug discovery for Huntington's DiseaseWolfgang Fecke
Siena Biotech S p A, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy
Drug Discov Today 14:453-64. 2009..Such discovery strategies have an impact on the configuration of screening cascades for effective translation of drug candidates toward clinical trials... - Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-Chiara Ghiron
Siena Biotech SpA, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy
J Med Chem 53:4379-89. 2010..Structural modifications leading to the improved selectivity profile and the biological evaluation of this series of compounds are discussed... - Robust MS quantification method for phospho-peptides using 18O/16O labelingClaus A Andersen
Siena Biotech SpA, Discovery Research, Via Fiorentina 1, 53100 Siena, Italy
BMC Bioinformatics 10:141. 2009..It was originally developed to study signaling cascades activated by amyloid-beta treatment of neurons used as a cellular model system with relevance to Alzheimer's disease, but is generally applicable... - Molecular cloning and initial characterization of the MG61/PORC gene, the human homologue of the Drosophila segment polarity gene PorcupineAndrea Caricasole
GlaxoSmithKline, Medicines Research Centre, Via Fleming 4, 37135 Verona, Italy
Gene 288:147-57. 2002..Finally, we present evidence indicating that MG61/PORC can influence the activity of a human Wnt7A expression construct in a T-cell factor-responsive reporter assay... - VSTM2L is a novel secreted antagonist of the neuroprotective peptide HumaninLara Rossini
Siena Biotech SpA, Strada del Petriccio e Belriguardo n 35, 53100 Siena, Italy
FASEB J 25:1983-2000. 2011..In summary, VSTM2L is the first example of a secreted antagonist of HN and may play a role in the modulation of HN biological functions... - Induction of Dickkopf-1, a negative modulator of the Wnt pathway, is associated with neuronal degeneration in Alzheimer's brainAndrea Caricasole
Siena Biotech, 53100 Siena, Italy
J Neurosci 24:6021-7. 2004..We conclude that induction of DKK1 contributes to the pathological cascade triggered by beta-amyloid and is critically involved in the process of tau phosphorylation... - Sequential detergent fractionation of primary neurons for proteomics studiesSimonetta Bernocco
Siena Biotech S p A, Discovery Research, Siena, Italy
Proteomics 8:930-8. 2008.... - Aryl azoles with neuroprotective activity--parallel synthesis and attempts at target identificationGiuseppe Cocconcelli
Siena Biotech S p A, Via Fiorentina 1, 53100 Siena, Italy
Bioorg Med Chem 16:2043-52. 2008..The compounds tested showed an activity between 40% and 70%. The identification of neuroprotective small molecules and the identification of NaV channels as the potential site of action were the most important goals of this work... - Pharmacological properties of rat alpha 7 nicotinic receptors expressed in native and recombinant cell systemsCaterina Virginio
Systems Research, GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135, Verona, Italy
Eur J Pharmacol 445:153-61. 2002.... - Differential inhibition of rat alpha3* and alpha7 nicotinic acetylcholine receptors by tetrandrine and closely related bis-benzylisoquinoline derivativesCaterina Virginio
GlaxoSmithKline Medicines Research Centre, Assay Development and Compound Profiling, Via A Fleming 4, 37135 Verona, Italy
Neurosci Lett 381:299-304. 2005..The different potencies and multiple modes of action on nAChRs may help to better understand the pharmacology of these receptors and to aid in novel drug design... - A primer on screening data managementMike Palmer
Siena Biotech S p A, Siena, Italy
J Biomol Screen 14:999-1007. 2009..It is also hoped that their experiences might provide an opportunity for reflection to data management practitioners operating in established environments... - Lithium induces gene expression through lymphoid enhancer-binding factor/T-cell factor responsive element in rat PC12 cellsEzio Bettini
Systems Research, GlaxoSmithKline Medicines Research Centre, Via A Fleming 4, 37135 Verona, Italy
Neurosci Lett 317:50-2. 2002..These results are consistent with the known inhibitory effects of lithium on GSK-3 and represent the first demonstration that a LEF/TCF responsive element also mediates lithium-induced gene expression in PC12 cells... - How to achieve confidence in drug discovery and development: managing risk (from a reductionist to a holistic approach)Annette Bakker
VP Portfolio Management, Siena Biotech SpA, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy
ChemMedChem 4:923-33. 2009.... - Molecular cloning and characterization of the human diacylglycerol kinase beta (DGKbeta) gene: alternative splicing generates DGKbeta isotypes with different propertiesAndrea Caricasole
GlaxoSmithKline Systems Research and Department of Biology, Via Fleming 4, 37135 Verona, Italy
J Biol Chem 277:4790-6. 2002..Therefore, the human diacylglycerol kinase beta gene can generate several enzyme isoforms, which can display different expression levels and subcellular localization but similar enzymatic activities in vitro... - Phosphoproteome analysisRoberto Raggiaschi
Sienabiotech S p A, Discovery Research, Siena, Italy
Biosci Rep 25:33-44. 2005..Moreover, methods to enrich phosphorylated proteins such as affinity chromatography (IMAC) and immunoprecipitation as well as mass spectrometry for identification of phosphorylated peptides and phosphorylation sites are also described... - A continuous time-resolved fluorescence assay for identification of BACE1 inhibitorsValentina Porcari
Sienabiotech S p A, Discovery Research, Siena, Italy
Assay Drug Dev Technol 3:287-97. 2005..The assay reproduced IC50 values of known inhibitors and detected them also as hits in a screening campaign. A high signal-to-noise ratio of 289 and a Z' factor of 0.76 make this assay suitable for high-throughput screening... - A bioinformatics perspective on proteomics: data storage, analysis, and integrationAndreas Kremer
Sienabiotech S p A, Discovery Research, Siena, Italy
Biosci Rep 25:95-106. 2005.... - Pharmacological and molecular characterisation of SK3 channels in the TE671 human medulloblastoma cell lineCorrado Carignani
GlaxoSmithKline Medicines Research Centre, Verona, Italy
Brain Res 939:11-8. 2002..3 nM. Furthermore, the current was significantly increased (132.6+/-5.2%, n=7) by 500 microM 1-ethyl-2-benzimidazolinone (EBIO). Collectively, these data demonstrate the presence of an endogenous SK3 channel in human TE671 cells... - Inhibition of the canonical Wnt signaling pathway by apolipoprotein E4 in PC12 cellsAlessandra Caruso
Department of Human Physiology and Pharmacology, University of Rome La Sapienza, Rome, Italy
J Neurochem 98:364-71. 2006..We conclude that ApoE4 behaves as an inhibitor of the canonical Wnt pathway in a context-independent manner... - In vitro screening strategies for nicotinic receptor ligandsJohn Dunlop
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543, USA
Biochem Pharmacol 74:1172-81. 2007.... - Functional characterization of WNT7A signaling in PC12 cells: interaction with A FZD5 x LRP6 receptor complex and modulation by Dickkopf proteinsAndrea Caricasole
Department of Human Physiology and Pharmacology, University of Rome La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy
J Biol Chem 278:37024-31. 2003..Our functional analysis indicates that WNT7A can specifically act via a Frizzled-5.LRP6 receptor complex in PC12 cells and that this activity can be antagonized by Dickkopf-1 and Dickkopf-3...