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Items: 1 to 50 of 68

1.

Generating Human iPSC-Derived Astrocytes with Chemically Defined Medium for In Vitro Disease Modeling.

Janssen K, Bahnassawy L, Kiefer C, Korffmann J, Terstappen GC, Lakics V, Cik M, Reinhardt P.

Methods Mol Biol. 2019;1994:31-39. doi: 10.1007/978-1-4939-9477-9_3.

PMID:
31124102
2.

Development of Human in vitro Brain-blood Barrier Model from Induced Pluripotent Stem Cell-derived Endothelial Cells to Predict the in vivo Permeability of Drugs.

Li Y, Sun X, Liu H, Huang L, Meng G, Ding Y, Su W, Lu J, Gong S, Terstappen GC, Zhang R, Zhang W.

Neurosci Bull. 2019 May 11. doi: 10.1007/s12264-019-00384-7. [Epub ahead of print]

PMID:
31079318
3.

Reproducibility of Molecular Phenotypes after Long-Term Differentiation to Human iPSC-Derived Neurons: A Multi-Site Omics Study.

Volpato V, Smith J, Sandor C, Ried JS, Baud A, Handel A, Newey SE, Wessely F, Attar M, Whiteley E, Chintawar S, Verheyen A, Barta T, Lako M, Armstrong L, Muschet C, Artati A, Cusulin C, Christensen K, Patsch C, Sharma E, Nicod J, Brownjohn P, Stubbs V, Heywood WE, Gissen P, De Filippis R, Janssen K, Reinhardt P, Adamski J, Royaux I, Peeters PJ, Terstappen GC, Graf M, Livesey FJ, Akerman CJ, Mills K, Bowden R, Nicholson G, Webber C, Cader MZ, Lakics V.

Stem Cell Reports. 2018 Oct 9;11(4):897-911. doi: 10.1016/j.stemcr.2018.08.013. Epub 2018 Sep 20.

4.

Prediction of brain:blood unbound concentration ratios in CNS drug discovery employing in silico and in vitro model systems.

Liu H, Dong K, Zhang W, Summerfield SG, Terstappen GC.

Drug Discov Today. 2018 Jul;23(7):1357-1372. doi: 10.1016/j.drudis.2018.03.002. Epub 2018 Mar 13. Review.

PMID:
29548981
5.

Drug Distribution into Peripheral Nerve.

Liu H, Chen Y, Huang L, Sun X, Fu T, Wu S, Zhu X, Zhen W, Liu J, Lu G, Cai W, Yang T, Zhang W, Yu X, Wan Z, Wang J, Summerfield SG, Dong K, Terstappen GC.

J Pharmacol Exp Ther. 2018 May;365(2):336-345. doi: 10.1124/jpet.117.245613. Epub 2018 Mar 6. Erratum in: J Pharmacol Exp Ther. 2018 Jul;366(1):237.

PMID:
29511033
6.

Quantitative Algorithm-Based Paired Imaging Measurement for Antibody-Triggered Endocytosis in Cultured Cells.

Gong S, Li Y, Su W, Ding Y, Lu J, Dong K, Hood S, Zhang W, Terstappen GC.

SLAS Discov. 2018 Sep;23(8):832-841. doi: 10.1177/2472555218761355. Epub 2018 Mar 5.

PMID:
29505735
7.

Brain delivery research in public-private partnerships: The IMI-JU COMPACT consortium as an example.

Meyer AH, Untucht C, Terstappen GC.

Neuropharmacology. 2017 Jul 1;120:8-10. doi: 10.1016/j.neuropharm.2016.06.012. Epub 2016 Jun 16. Review.

PMID:
27318272
8.

Label-free detection of small-molecule binding to a GPCR in the membrane environment.

Heym RG, Hornberger WB, Lakics V, Terstappen GC.

Biochim Biophys Acta. 2015 Aug;1854(8):979-86. doi: 10.1016/j.bbapap.2015.04.003. Epub 2015 Apr 14.

PMID:
25882196
9.

Targeting mutant huntingtin for the development of disease-modifying therapy.

Appl T, Kaltenbach L, Lo DC, Terstappen GC.

Drug Discov Today. 2012 Nov;17(21-22):1217-23. doi: 10.1016/j.drudis.2012.06.017. Epub 2012 Jul 4. Review.

PMID:
22772050
10.

Heterocomplex formation of 5-HT2A-mGlu2 and its relevance for cellular signaling cascades.

Delille HK, Becker JM, Burkhardt S, Bleher B, Terstappen GC, Schmidt M, Meyer AH, Unger L, Marek GJ, Mezler M.

Neuropharmacology. 2012 Jun;62(7):2184-91. doi: 10.1016/j.neuropharm.2012.01.010. Epub 2012 Jan 25.

PMID:
22300836
11.

Development and validation of a fluorescence-based HTS assay for the identification of P/Q-type calcium channel blockers.

Mezler M, Hermann D, Swensen AM, Draguhn A, Terstappen GC, Gross G, Schoemaker H, Freiberg G, Pratt S, Gopalakrishnan SM, Nimmrich V.

Comb Chem High Throughput Screen. 2012 Jun 1;15(5):372-85.

PMID:
22272661
12.

Preclinical assessment of an adjunctive treatment approach for cognitive impairment associated with schizophrenia using the alpha7 nicotinic acetylcholine receptor agonist WYE-103914/SEN34625.

Marquis KL, Comery TA, Jow F, Navarra RL, Grauer SM, Pulicicchio C, Kelley C, Brennan JA, Roncarati R, Scali C, Haydar S, Ghiron C, Terstappen GC, Dunlop J.

Psychopharmacology (Berl). 2011 Dec;218(4):635-47. doi: 10.1007/s00213-011-2357-6. Epub 2011 Jun 4.

PMID:
21643676
13.

Screening technologies for ion channel drug discovery.

Terstappen GC, Roncarati R, Dunlop J, Peri R.

Future Med Chem. 2010 May;2(5):715-30. doi: 10.4155/fmc.10.180. Review.

PMID:
21426199
14.

VSTM2L is a novel secreted antagonist of the neuroprotective peptide Humanin.

Rossini L, Hashimoto Y, Suzuki H, Kurita M, Gianfriddo M, Scali C, Roncarati R, Franceschini D, Pollio G, Trabalzini L, Terstappen GC, Matsuoka M, Caricasole A.

FASEB J. 2011 Jun;25(6):1983-2000. doi: 10.1096/fj.10-163535. Epub 2011 Mar 10.

PMID:
21393573
15.

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-103914).

Ghiron C, Haydar SN, Aschmies S, Bothmann H, Castaldo C, Cocconcelli G, Comery TA, Di L, Dunlop J, Lock T, Kramer A, Kowal D, Jow F, Grauer S, Harrison B, La Rosa S, Maccari L, Marquis KL, Micco I, Nencini A, Quinn J, Robichaud AJ, Roncarati R, Scali C, Terstappen GC, Turlizzi E, Valacchi M, Varrone M, Zanaletti R, Zanelli U.

J Med Chem. 2010 Jun 10;53(11):4379-89. doi: 10.1021/jm901692q.

PMID:
20465311
16.

Endothelial cell adhesion to the extracellular matrix induces c-Src-dependent VEGFR-3 phosphorylation without the activation of the receptor intrinsic kinase activity.

Galvagni F, Pennacchini S, Salameh A, Rocchigiani M, Neri F, Orlandini M, Petraglia F, Gotta S, Sardone GL, Matteucci G, Terstappen GC, Oliviero S.

Circ Res. 2010 Jun 25;106(12):1839-48. doi: 10.1161/CIRCRESAHA.109.206326. Epub 2010 Apr 29.

PMID:
20431062
17.

Increased Dickkopf-1 expression in transgenic mouse models of neurodegenerative disease.

Rosi MC, Luccarini I, Grossi C, Fiorentini A, Spillantini MG, Prisco A, Scali C, Gianfriddo M, Caricasole A, Terstappen GC, Casamenti F.

J Neurochem. 2010 Mar;112(6):1539-51. doi: 10.1111/j.1471-4159.2009.06566.x. Epub 2009 Dec 29.

18.

A primer on screening data management.

Palmer M, Kremer A, Terstappen GC.

J Biomol Screen. 2009 Sep;14(8):999-1007. doi: 10.1177/1087057109341767. Epub 2009 Jul 30. Review.

PMID:
19643981
19.

How to achieve confidence in drug discovery and development: managing risk (from a reductionist to a holistic approach).

Bakker A, Caricasole A, Gaviraghi G, Pollio G, Robertson G, Terstappen GC, Salerno M, Tunici P.

ChemMedChem. 2009 Jun;4(6):923-33. doi: 10.1002/cmdc.200900056.

PMID:
19434656
20.

Robust MS quantification method for phospho-peptides using 18O/16O labeling.

Andersen CA, Gotta S, Magnoni L, Raggiaschi R, Kremer A, Terstappen GC.

BMC Bioinformatics. 2009 May 11;10:141. doi: 10.1186/1471-2105-10-141.

21.

Small molecule drug discovery for Huntington's Disease.

Fecke W, Gianfriddo M, Gaviraghi G, Terstappen GC, Heitz F.

Drug Discov Today. 2009 May;14(9-10):453-64. doi: 10.1016/j.drudis.2009.02.006. Epub 2009 Feb 25. Review.

PMID:
19429504
22.

Not a dilemma: target deconvolution in drug discovery.

Terstappen GC.

Future Med Chem. 2009 Apr;1(1):7-9. doi: 10.4155/fmc.09.3. No abstract available.

23.

Procognitive and neuroprotective activity of a novel alpha7 nicotinic acetylcholine receptor agonist for treatment of neurodegenerative and cognitive disorders.

Roncarati R, Scali C, Comery TA, Grauer SM, Aschmi S, Bothmann H, Jow B, Kowal D, Gianfriddo M, Kelley C, Zanelli U, Ghiron C, Haydar S, Dunlop J, Terstappen GC.

J Pharmacol Exp Ther. 2009 May;329(2):459-68. doi: 10.1124/jpet.108.150094. Epub 2009 Feb 17.

PMID:
19223665
24.

Drug discovery and development for Huntington's disease - an orphan indication with high medical need.

Heitz F, La Rosa S, Gonzalez-Couto E, Gaviraghi G, Terstappen GC.

IDrugs. 2008 Sep;11(9):653-60. Review.

PMID:
18763216
25.

Molecular cloning and characterization of a novel human variant of RIC-3, a putative chaperone of nicotinic acetylcholine receptors.

Seredenina T, Ferraro T, Terstappen GC, Caricasole A, Roncarati R.

Biosci Rep. 2008 Dec;28(6):299-306. doi: 10.1042/BSR20080055.

PMID:
18691158
26.

Increased expression of the oligopeptidase THOP1 is a neuroprotective response to Abeta toxicity.

Pollio G, Hoozemans JJ, Andersen CA, Roncarati R, Rosi MC, van Haastert ES, Seredenina T, Diamanti D, Gotta S, Fiorentini A, Magnoni L, Raggiaschi R, Rozemuller AJ, Casamenti F, Caricasole A, Terstappen GC.

Neurobiol Dis. 2008 Jul;31(1):145-58. doi: 10.1016/j.nbd.2008.04.004. Epub 2008 Apr 29.

PMID:
18571100
27.

Functional screening of α7 nicotinic receptor ligands.

Dunlop J, Peri R, Terstappen GC, Bowlby M.

Expert Opin Drug Discov. 2008 Jun;3(6):623-8. doi: 10.1517/17460441.3.6.623.

PMID:
23506144
28.

A reporter assay for target validation in primary neuronal cultures.

Pollio G, Roncarati R, Seredenina T, Terstappen GC, Caricasole A.

J Neurosci Methods. 2008 Jul 15;172(1):34-7. doi: 10.1016/j.jneumeth.2008.03.018. Epub 2008 Apr 7.

PMID:
18485484
29.

Functional properties of alpha7 nicotinic acetylcholine receptors co-expressed with RIC-3 in a stable recombinant CHO-K1 cell line.

Roncarati R, Seredenina T, Jow B, Jow F, Papini S, Kramer A, Bothmann H, Dunlop J, Terstappen GC.

Assay Drug Dev Technol. 2008 Apr;6(2):181-93. doi: 10.1089/adt.2007.120.

PMID:
18471073
30.

Sequential detergent fractionation of primary neurons for proteomics studies.

Bernocco S, Fondelli C, Matteoni S, Magnoni L, Gotta S, Terstappen GC, Raggiaschi R.

Proteomics. 2008 Mar;8(5):930-8. doi: 10.1002/pmic.200700738.

PMID:
18219698
31.

Aryl azoles with neuroprotective activity--parallel synthesis and attempts at target identification.

Cocconcelli G, Diodato E, Caricasole A, Gaviraghi G, Genesio E, Ghiron C, Magnoni L, Pecchioli E, Plazzi PV, Terstappen GC.

Bioorg Med Chem. 2008 Feb 15;16(4):2043-52. Epub 2007 Nov 4.

PMID:
18024137
32.

Target deconvolution strategies in drug discovery.

Terstappen GC, Schlüpen C, Raggiaschi R, Gaviraghi G.

Nat Rev Drug Discov. 2007 Nov;6(11):891-903. Review.

PMID:
17917669
33.

In vitro screening strategies for nicotinic receptor ligands.

Dunlop J, Roncarati R, Jow B, Bothmann H, Lock T, Kowal D, Bowlby M, Terstappen GC.

Biochem Pharmacol. 2007 Oct 15;74(8):1172-81. Epub 2007 Jul 10.

PMID:
17706607
34.

Inhibition of Wnt signaling, modulation of Tau phosphorylation and induction of neuronal cell death by DKK1.

Scali C, Caraci F, Gianfriddo M, Diodato E, Roncarati R, Pollio G, Gaviraghi G, Copani A, Nicoletti F, Terstappen GC, Caricasole A.

Neurobiol Dis. 2006 Nov;24(2):254-65. Epub 2006 Aug 17.

PMID:
16919965
35.

Inhibition of the canonical Wnt signaling pathway by apolipoprotein E4 in PC12 cells.

Caruso A, Motolese M, Iacovelli L, Caraci F, Copani A, Nicoletti F, Terstappen GC, Gaviraghi G, Caricasole A.

J Neurochem. 2006 Jul;98(2):364-71.

36.

The Wnt signaling pathway as a target for the treatment of neurodegenerative disorders.

Terstappen GC, Gaviraghi G, Caricasole A.

IDrugs. 2006 Jan;9(1):35-8.

PMID:
16374731
37.

Detection of phosphorylation patterns in rat cortical neurons by combining phosphatase treatment and DIGE technology.

Raggiaschi R, Lorenzetto C, Diodato E, Caricasole A, Gotta S, Terstappen GC.

Proteomics. 2006 Feb;6(3):748-56.

PMID:
16372257
38.

Two sides of the same coin: Wnt signaling in neurodegeneration and neuro-oncology.

Caricasole A, Bakker A, Copani A, Nicoletti F, Gaviraghi G, Terstappen GC.

Biosci Rep. 2005 Oct-Dec;25(5-6):309-27. Review.

PMID:
16307379
39.

A bioinformatics perspective on proteomics: data storage, analysis, and integration.

Kremer A, Schneider R, Terstappen GC.

Biosci Rep. 2005 Feb-Apr;25(1-2):95-106. Review.

PMID:
16222422
40.

Phosphoproteome analysis.

Raggiaschi R, Gotta S, Terstappen GC.

Biosci Rep. 2005 Feb-Apr;25(1-2):33-44. Review.

PMID:
16222418
41.

Ion channel screening technologies today.

Terstappen GC.

Drug Discov Today Technol. 2005 Summer;2(2):133-40. doi: 10.1016/j.ddtec.2005.05.011.

PMID:
24981840
42.

A continuous time-resolved fluorescence assay for identification of BACE1 inhibitors.

Porcari V, Magnoni L, Terstappen GC, Fecke W.

Assay Drug Dev Technol. 2005 Jun;3(3):287-97.

PMID:
15971990
43.
44.

Nonradioactive rubidium ion efflux assay and its applications in drug discovery and development.

Terstappen GC.

Assay Drug Dev Technol. 2004 Oct;2(5):553-9. Review.

PMID:
15671653
45.

Induction of Dickkopf-1, a negative modulator of the Wnt pathway, is associated with neuronal degeneration in Alzheimer's brain.

Caricasole A, Copani A, Caraci F, Aronica E, Rozemuller AJ, Caruso A, Storto M, Gaviraghi G, Terstappen GC, Nicoletti F.

J Neurosci. 2004 Jun 30;24(26):6021-7.

46.

Functional characterization of WNT7A signaling in PC12 cells: interaction with A FZD5 x LRP6 receptor complex and modulation by Dickkopf proteins.

Caricasole A, Ferraro T, Iacovelli L, Barletta E, Caruso A, Melchiorri D, Terstappen GC, Nicoletti F.

J Biol Chem. 2003 Sep 26;278(39):37024-31. Epub 2003 Jul 11.

47.

The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3.

Terstappen GC, Pellacani A, Aldegheri L, Graziani F, Carignani C, Pula G, Virginio C.

Neurosci Lett. 2003 Jul 31;346(1-2):85-8.

PMID:
12850554
48.

The Wnt pathway, cell-cycle activation and beta-amyloid: novel therapeutic strategies in Alzheimer's disease?

Caricasole A, Copani A, Caruso A, Caraci F, Iacovelli L, Sortino MA, Terstappen GC, Nicoletti F.

Trends Pharmacol Sci. 2003 May;24(5):233-8. Review.

PMID:
12767722
49.

Pharmacological properties of rat alpha 7 nicotinic receptors expressed in native and recombinant cell systems.

Virginio C, Giacometti A, Aldegheri L, Rimland JM, Terstappen GC.

Eur J Pharmacol. 2002 Jun 12;445(3):153-61.

PMID:
12079679
50.

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