HTS techniques for patch clamp-based ion channel screening - advances and economy
Farre C and Fertig N
Expert Opin. Drug Disc. early online publication April 2012
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User publication: 'Selective modification of the N-Terminal structure of polytheonamide B significantly changes its cytotoxicity and activity as an ion channel'
Shinohara N, Itoh H, Matsuoka S, and Inoue M
ChemMedChem, published online April 4th, 2012
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User Publication: 'Calcium regulation by thermo- and osmosensing transient receptor potential vanilloid channels (TRPVs) in human conjunctival epithelial cells'
Stefan Mergler, Fabian Garreis, Monika Sahlmüller, Ekaterini-Maria Lyras,
Peter S. Reinach, Abhilash Dwarakanath, Friedrich Paulsen, Uwe Pleyer
Histochem. Cell. Biol., Published online February 12 2012
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Nanopore-based single-molecule mass spectrometry on a lipid membrane microarray
Baaken G., Ankri N., Schuler A.K., Rühe J., Behrends C.
Am. Chem. Soc Nano, 5(10), 8080-8088, 2011
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User publication: 'Functional analysis of synthetic substructures of polytheonamide B: A transmembrane channel-forming peptide'
Matsuoka S, Shinohara N, Takahashi T, Iida M, and Inoue M
Angew. Chem. Int. Ed., 50, 4879 – 4883, 2011
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User Publication: 'Green fluorescent protein changes the conductance of connexon 43 hemichannels reconstituted in planar lipid bilayers'
Christian Carnarius , Mohamed Kreir, Marcel Krick, Christoph Methfessel, Volker Moehrle, Oliver Valerius, Andrea Brüggemann, Claudia Steinem, Niels Fertig
Journal of Biological Chemistry, Published on December 3, 2011 as Manuscript M111.319871
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State-of-the-art automated patchclamp devices: heatactivation, actionpotentials, and highthroughput in ionchannel screening
Sonja Stoelzle, Alison Obergrussberger, Andrea Brüggemann, Claudia Haarmann, Michael George, Ralf Kettenhofen and Niels Fertig
Frontiers in Pharmacology, November 2011, Volume 2 , Article 76
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User Review: 'Automated electrophysiology makes the pace for cardiac ion channel safety screening'
Clemens Möller, Harry Witchel
Frontiers in Pharmacology, November 2011, Volume 2, Article 73
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User Publication: 'Thermo-sensitive transient receptor potential vanilloid channel-1 regulates intracellular calcium and triggers chromogranin A secretion in pancreatic neuroendocrine BON-1 tumor cells'
Stefan Mergler, Marek Skrzypski, Maciej Sassek, Piotr Pietrzak, Christina Pucci, Bertram Wiedenmann, Mathias Z. Strowski
Cellular Signalling 24 (2012) 233–246
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User Publication: 'Characterization of transient receptor potential vanilloid channel 4 (TRPV4) in human corneal endothelial cells'
Stefan Mergler,, Monika Valtink, Katrin Taetz, Monika Sahlmüller, Gabriele Fels, Peter S. Reinach, Katrin Engelmann and Uwe Pleyer
Experimental Eye Research 93 (2011) 710e719
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Chimeric approach reveals that differences in the TRPV1 pore domain determine species-specific sensitivity to block of heat activation
Papakosta M., Dalle C., Haythornthwaite A., Cao L., Stevens E.B., Burgess G., Russell R., Cox P.J., Phillips S.C., Grimm C.
J. Biol. Chem., 2011 Sep 12. [Epub ahead of print]
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User Publication: 'Thermosensitive transient receptor potential channels in human corneal epithelial cells'
Mergler S., Garreis F., Sahlmüller M., Reinach P.S., Paulsen F., and Pleyer U.
J. Cell. Physiol., 2011, 226, 1828 - 1842
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User Publication: 'Physiologie des humanen Hornhautendothels - neue Erkenntnisse durch elektrophysiologische Untersuchungen'
Mergler S. and Pleyer U.
Klin. Monatsbl. Augenheilkd., 2011, 228, 520 - 524
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User Publication: 'Rapid and Contrasting Effects of Rosiglitazone on Transient Receptor Potential TRPM3 and TRPC5 Channels'
Majeed Y, Bahnasi Y, Seymour VAL, Wilson LA, Milligan CJ, Agarwal AK, Sukumar P, Naylor J, and
Beech DJ
Mol. Pharmacol., 79(6),1023-30, 2011
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Automated Patch Clamp on mESC-Derived Cardiomyocytes for Cardiotoxicity Prediction
Stoelzle S, Haythornthwaite A, Kettenhofen R, Kolossov E, Bohlen H, George M, Brüggemann A, Fertig N.
J Biomol Screen. 2011 Jul 20. [Epub ahead of print]
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Voltage-gated sodium channel (NaV) protein dissection creates a set of functional pore-only proteins
David Shaya, Mohamed Kreir, Rebecca A. Robbins, Stephanie Wong, Justus Hammon, Andrea Brüggemann, and Daniel L. Minor, Jr
PNAS Early Edition, 2011, 1 - 6
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User Publication: 'Pharmacological studies of Cav3.1 T-type calcium channels using automated patch-clamp techniques'
Kee-Hyun Choi, Chiman Song, Chan S. Cheong and Hyewhon Rhim
Gen. Physiol. Biophys., 2011, 30, 100–105
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User Publication: 'Chemical and biological characterization of four new linear cationic a-helical peptides from the venoms of two solitary eumenine wasps'
Marisa Rangel, Marcia Perez dos Santos Cabrera, Kohei Kazuma, Kenji Ando, Xiaoyu Wang, Manabu Kato, Ken-ichi Nihei, Izaura Yoshico Hirata, Tyra J. Cross, Angélica Nunes Garcia, Eliana L. Faquim-Mauro, Marcia Regina Franzolin, Hiroyuki Fuchino, Kanami Mori-Yasumoto, Setsuko Sekita, Makoto Kadowaki, Motoyoshi Satake, Katsuhiro Konno
Toxicon 2011, 57,1081–1092
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Book chapter: 'Cardiac Toxicity'
Ralf Kettenhofen and Silke Schwengberg
ADMET for Medicinal Chemists: A Practical Guide, Edited by Katya Tsaioun and Steven A. Kates, John Wiley & Sons, Inc., 2011, 287 - 314 |
User Publication: 'Development of a selective small-molecule inhibitor of Kir1.1, the Renal Outer Medullary Potassium Channel'
Gautam Bhave1, Brian A. Chauder1, Wen Liu2, Eric S. Dawson1, Rishin Kadakia1, Thuy T. Nguyen1, L. Michelle Lewis1, Jens Meiler1, C. David Weaver1, Lisa M. Satlin2, Craig W. Lindsley1 and Jerod S. Denton1,
Molecular Pharmacology, 2011, 79(1), 42-50 |
Propranolol blocks cardiac and neuronal voltage-gated sodium channels
Dao W. Wang, Akshitkumar M. Mistry, Kristopher M. Kahlig, Jennifer A. Kearney, Jizhou Xiang and Alfred L. George Jr., Frontiers in Pharmacology, Original Research Article published: 31 December 2010; doi: 10.3389/fphar.2010.00144
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Cor.At® Cardiomyocytes: Primary-like Cardiomyocytes for Manual and Automated Electrophysiological Screening
 Ralf Kettenhofen1 and Sonja Stoelzle2, 1Axiogenesis AG, Cologne, Germany, 2Nanion Technologies, Munich, Germany
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Characterization of two pore channel 2 (TPCN2)-mediated Ca2+ currents in isolated lysosomes
 Schieder M., Rötzer K., Brüggemann A., Biel M. and Wahl-Schott C.A.: The Journal of Biological Chemistry Vol. 285, No. 28, pp. 21219–21222, July 9, 2010
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User Publication: 'Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae'
Balansa W, Islam R, Fontaine F, Piggott AM, Zhang H, Webb TI, Gilbert DF, Lynch JW, Capon RJ. Bioorg Med Chem. 2010 Apr 15;18(8):2912-9. Epub 2010 Mar 6.
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User Publication: 'TRPV channels mediate temperature-sensing in human corneal endothelial cells'
Stefan Mergler, Monika Valtink, Vivien Jane Coulson-Thomas, Dirk Lindemann, Peter S. Reinach, Katrin Engelmanng, Uwe Pleyer,
Experimental Eye Research 90 (2010) 758e770
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Editorial: 'Renaissance of ion channel research and drug discovery by patch clamp automation'
Farre C. and Fertig N. Future Med. Chem., 2010, 2(5), 1-5. |
User Publication: 'Pregnenolone Sulphate- and Cholesterol-Regulated TRPM3 Channels Coupled to Vascular Smooth Muscle Secretion and Contraction'
Naylor J., Li J., Milligan C.J, Zeng F., Sukumar P., Hou B., Sedo A., Yuldasheva N., Majeed Y., Beri D., Jiang S., Seymour V.A.L, McKeown L., Kumar B., Harteneck C., O'Regan D., Wheatcroft S.B., Kearney M.T, Jones C., Porter K.E. and Beech D.J. Circ. Res., 2010, published online Apr 10, 1-18. |
User Publication: 'Multiplexed transposon-mediated stable gene transfer in human cells'
Kahlig K.M., Saridey S.K., Kaja A., Daniels M.A., George A.L. Jr and Wilson M.H. Proc. Natl. Acad. Sci. USA., 2010, Jan 26;107(4), 1343-8. |
User Publication: 'Permeation of antibiotics through escherichia coli OmpF and OmpC porins: screening for influx on a single-molecule level'
Mahendran K.R., Kreir M., Weingart H., Fertig N., Winterhalter M. J. Biomol. Screen., 2010 Jan 19
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User Publication: 'Studying mechanosensitive ion channels using liposomes'
Martinac B., Rohde P.R., Battle A. R., Petrov E., Pal P, Alexander Foo A.FW, Vásquez V., Huynh T. and Kloda A.
Methods Mol. Biol. 2010, 606, 31-53. |
User Publication: 'High throughput techniques for discovering new glycine receptor modulators and their binding sites'
Gilbert D.F.,Islam R., Lynagh T., Lynch J.W., Webb T.I. Front.
Mol. Neurosci., 2009, 2(17), 1-10. Epub 2009 Oct 30 |
User Publication: 'High-throughput screening reveals a small-molecule inhibitor of the renal outer medullary potassium channel and Kir7.1'
Lewis L.M., Bhave G., Chauder B.A., Banerjee S., Lornsen K.A., Redha R., Fallen K., Lindsley C.W., Weaver C.D.,
Denton J. Mol. Pharmacol., 2009, 76(5), 1094-1103.
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User Publication: 'The M34A mutant of Connexin26 reveals active conductance states in pore-suspending membranes'
Gaßmann O., Kreir M., Ambrosi C., Pranskevich J., Oshima A, Röling C., Sosinsky G., Fertig N., Steinem C.
Journal of Structural Biology, 2009, 168 (1), 168-176.
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User Publication: 'Transient receptor potential ankyrin 1 antagonists block the noxious effects of toxic industrial isocyanates and tear gases'
Bessac B.F., Sivula M., von Hehn C.A., Caceres A.I., Escalera, J, Jordt S.
FASEB Journal, 2009; 23, 1102-1114. |
User Publication: 'Amyloid-beta-Induced Ion Flux in Artificial Lipid Bilayers and Neuronal Cells: Resolving a Controversy'
Capone R., Quiroz F.G., Prangkio P., Saluja I., Sauer A.M., Bautista M.R., Turner R.S., Yang J., Mayer M.
Neurotox. Res., 2009, 16(1), 1-13. Epub 2009 Mar 19.
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User Publication: 'Robotic multiwell planar patch-clamp for native and primary mammalian cells'
Milligan C.J., Li J., Sukumar P., Majeed Y., Dallas M.L., English A., Emery P., Porter K.E., Smith A.M., McFadzean I.,
Beccano-Kelly D., Bahnasi Y., Cheong A., Naylor J., Zeng F., Liu X., Gamper N., Jiang L., Pearson H.A., Peers C., Robertson B., Beech D.J.
Nature Protocols, 2009, 4(2), 244-255. See more
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'Ion channel screening – automated patch clamp on the rise'
Farre C., George M., Brüggemann A., Fertig N.
Drug Discovery Technology, 2009,
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'Port-a-Patch and Patchliner: High fidelity electrophysiology for secondary screening and safety pharmacology'
Farre C., Haythornthwaite A., Haarmann C., Stoelzle S., Kreir M., George M., Brüggemann A., Fertig N.
Comb. Chem. & HTS, 2009, 12 (1), 24-37.
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User Publication:'T-type channel blocking properties and antiabsence activity of two imidazo[1,2-b]pyridazine derivatives structurally related to indomethacin'
Rimoli M.G., Russo E., Cataldi M., Citraro R., Ambrosino P., Melisi D., Curcio A., De Lucia S., Patrignani P., De Sarro G., Abignente E.
Neuropharmacology, 2008, Nov 30., E-publication ahead of print.
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'Rapid screening of membrane protein activity: electrophysiological analysis of OmpF reconstituted in proteoliposomes'
Kreir M., Farre C., Beckler M., George M., Fertig N.
Lab-on-a-Chip, 2008, 8(4), 587-95.
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Book chapter: 'Planar patch clamp – Advances in electrophysiology'
Brüggemann A., Farre C., Haarmann C., Haythornthwaite A., Kreir M., Stoelzle S., George M., Fertig N.
Methods in Molecular Biology, Potassium channels, Humana Press, 2008, 49, 165-176.
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'Planar patch-clamp force microscopy on living cells'
Pamir E., George M., Fertig N., Benoit M.
Ultramicroscopy, 2008, 108(6), 552-557.
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User Publication: 'Interactions, functions, and independence of plasma membrane STIM1 and TRPC1 in vascular smooth muscle cells'
Li J., Sukumar P., Milligan C.J., Kumar B., Ma Z.Y., Munsch C.M., Jiang L.H., Porter K.E., Beech D.J.
Circ. Res., 2008 103(8), e97-104.
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User Publication: 'Production of a specific extracellular inhibitor of TRPM3 channels'
Naylor J., Milligan C.J., Zeng F., Jones C., Beech D.J.
British Journal of Pharmacology, 2008, 1–7.
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User Publication: 'TRPC channel activation by extracellular thioredoxin'
Xu S.Z., Sukumar P., Zeng F., Li J., Jairaman A., English A., Naylor J., Ciurtin C., Majeed Y., Milligan C.J., Bahnasi Y.M., Al-Shawaf E., Porter K.E., Jiang L.H., Emery P., Sivaprasadarao A., Beech D.J.
Nature, 2008 451(7174), 69-72.
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User Publication: 'Planar Patch-Clamp Force Microscopy on Living Cells'
Pamir E., George M., Feritg, N., Benoit M., 2008, 108, 552-557.
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User review of planar electrophysiological devices: 'High-throughput electrophysiology: an emerging paradigm for ion-channel screening and physiology'
Dunlop J., Bowlby M., Peri R., Vasilyev D., Arias R.
Nature Reviews Drug Discovery, 2008, 7, 358-368. |
User Publication: 'TRPA1 is a major oxidant sensor in murine airway sensory neurons'
Bessac B.F., Sivula M., von Hehn C.A., Escalera J., Cohn L., Jordt S.E.
J. Clin. Invest., 2008, 118(5), 1899-1910
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User Publication: 'Synthesis and biological evaluation of chalcones as inhibitors of the voltage-gated potassium channel Kv1.3'
Cianci J., Baell J.B., Flynn B.L., Gable R.W., Mould J.A., Paul D., Harvey A.J.
Bioorganic & Med. Chem. Lett., 2008, 18, 2055–2061. |
'Rapid screening of membrane protein activity: electrophysiological analysis of OmpF reconstituted in proteoliposomes'
Kreir M., Farre C., Beckler M., George M., Fertig N.
Lab-on-a-Chip, 2008, 8(4), 587-95.
Download PDF-file (306 kB) |
User Publication: 'Electrophysiological assessment of HERG blockade: Comparative study using automated and conventional patch clamp systems'
Yook Y., Kim J., Cho H., Moon H., Kwak B.
Toxicology Letters, 2007, 172 (Suppl.1), S98-S99. |
Book chapter: 'Planar Patch Clamping'
Behrends, J.C., Fertig, N.
Patch Clamp Analysis – Advanced Techniques, Series: Neuromethods, Springer, 2007, 38, 411-433.
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'Automated ion channel screening: patch clamping made easy'
Farre C., Stoelzle S., Haarman C., George M., Brueggemann A., Fertig N.
Expert Opinion Therapeutic Targets, 2007, 11(4), 557-565.
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'Microchip technology for automated and parallel patch clamp recording'
Brüggemann A., Stoelzle S., George M., Behrends J.C., Fertig N.
Small, 2006, 2(7), 840 – 846.
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'High-resolution electrophysiology on a chip: Transient dynamics of alamethicin channel formation'
Sondermann M., George M., Fertig N., Behrends J.C.
Biochimica et Biophysica Acta 1758, 2006, 545–551.
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'Cytotoxicity of colloidal CdSe and CdSe/ZnS nanoparticles'
Kirchner C., Liedl T., Kudera S., Pellegrino T., Munoz J. A., Gaub H.E., Stoelzle S., Fertig N., Parak W.J.
Nano Lett., 2005, 5(2), 331-338.
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'The Port-a-Patch: The smallest patch clamp set up for high quality electrophysiology'
Brüggemann A., George M., Klau M., Beckler M., Steindl J., Behrends J., Fertig N.
HEKA impulse 03, 2005, 2-4.
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'Ion channel drug discovery and research: The automated Nano-Patch-Clamp technology'
Brüggemann A., George M., Klau M., Beckler M., Steindl J., Behrends J.C., Fertig N.
Current Drug Discovery Technologies, 2004, 1(1), 91-96.
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'High quality ion channel analysis on a chip with the NPC-technology'
Brüggemann A., George M., Klau M., Beckler M., Steindl J., Behrends J.C., Fertig N.
Assay and Drug Development Technologies, 2003, 1(5), 665-673.
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'Microstructured apertures in planar glass substrates for ion channel research'
Fertig N., Meyer C., Tilke A., George M., Klau M., Sobotta C., Blick R.H., Behrends J.C.
Channels and Receptors, 2003, 9(1), 29-40. |
'Simultaneous optical and electrical recording of single gramicidin channels'
Borisenko V., Lougheed L., Hesse J., Fuereder-Kitzmueller E., Fertig N., Behrends, J.C., Woolley G.A., Schuetz G.J.
Biophys. J., 2003, 84, 612-622.
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'Activity of single ion channel proteins detected with a planar microstructure'
Fertig N., Klau M., George M., Blick R.H., Behrends J.C.
APL, 2002, 81(25), 4865-67.
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'Microstructured glass chip for ion channel electrophysiology'
Fertig N., Meyer C., Blick R.H., Trautmann C., Behrends J.C. Physical Review E, 2001, 64, 040901 R.
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Stable integration of isolated cell membrane patches in a nanomachined aperture: A step towards a novel device for membrane physiology'
Fertig N., Tilke A., Blick R.H., Kotthaus J.P., Behrends J.C., ten Bruggencate G.
APL, 2000, 77(8), 1218-20.
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Michael Schieder, Katrin Rötzer, Andrea Brüggemann, Martin Biel and Christian Wahl-Schott
