Drug- and ion channel screening (Roboocyte)

Bah GS, Schneckener S, Hahnel SR, Bayang NH, Fieseler H, Schmuck GM, Krebber R, Sarr A, Terjung C, Ngangyung HF, Ekale DD, Mfopit YM, Rufener L, Graham-Brown J, Tanya VN, Glenschek-Sieberth M, Kulke D, Makepeace BL (2021) Emodepside targets SLO-1 channels of Onchocerca ochengi and induces broad anthelmintic effects in a bovine model of onchocerciasis. PLoS Pathog 17:e1009601.

Epstein M, Bali K, Piggot TJ, Green AC, Timperley CM, Bird M, Tattersall JEH, Bermudez I, Biggin PC (2021) Molecular determinants of binding of non-oxime bispyridinium nerve agent antidote compounds to the adult muscle nAChR. Toxicology Letters 340:114-122.

Gubič Š, Hendrickx LA, Toplak Ž, Sterle M, Peigneur S, Tomašič T, Pardo LA, Tytgat J, Zega A, Mašič LP (2021) Discovery of K(V) 1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges. Med Res Rev.

Hipp JF, Knoflach F, Comley R, Ballard TM, Honer M, Trube G, Gasser R, Prinssen E, Wallace TL, Rothfuss A, Knust H, Lennon-Chrimes S, Derks M, Bentley D, Squassante L, Nave S, Nöldeke J, Wandel C, Thomas AW, Hernandez MC (2021) Basmisanil, a highly selective GABA(A)-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man. Sci Rep 11:7700.

Lemel L, Nieścierowicz K, García-Fernández MD, Darré L, Durroux T, Busnelli M, Pezet M, Rebeille F, Jouhet J, Mouillac B, Domene C, Chini B, Cherezov V, Moreau CJ (2021) The ligand-bound state of a G protein-coupled receptor stabilizes the interaction of functional cholesterol molecules. J Lipid Res:100059.

Minguez-Viñas T, Nielsen BE, Shoemark DK, Gotti C, Sessions RB, Mulholland AJ, Bouzat C, Wonnacott S, Gallagher T, Bermudez I, Oliveira AS (2021) A conserved arginine with non-conserved function is a key determinant of agonist selectivity in α7 nicotinic acetylcholine receptors. British Journal of Pharmacology n/a.

Schwarz N, Seiffert S, Pendziwiat M, Rademacher A, Brünger T, Hedrich UBS, Augustijn PB, Baier H, Bayat A, Bisulli F, Buono RJ, Bruria BZ, Doyle MG, Guerrini R, Heimer G, Iacomino M, Kearney H, Klein KM, Kousiappa I, Kunz WS, Lerche H, Licchetta L, Lohmann E, Minardi R, McDonald M, Montgomery S, Mulahasanovic L, Oegema R, Ortal B, Papacostas SS, Ragona F, Granata T, Reif PS, Rosenow F, Rothschild A, Scudieri P, Striano P, Tinuper P, Tanteles GA, Vetro A, Zahnert F, Zara F, Lal D, May P, Muhle H, Helbig I, Weber Y (2021) Heterozygous variants in KCNC2 cause a broad spectrum of epilepsy phenotypes associated with characteristic functional alterations. medRxiv:2021.2005.2021.21257099.

Sridhar A, Lummis SCR, Pasini D, Mehregan A, Brams M, Kambara K, Bertrand D, Lindahl E, Howard RJ, Ulens C (2021) A cationic lipid site at the outward transmembrane face of a pentameric ligand-gated ion channel. bioRxiv:2021.2003.2024.436810.

Sridhar A, Lummis SCR, Pasini D, Mehregan A, Brams M, Kambara K, Bertrand D, Lindahl E, Howard RJ, Ulens C (2021) Regulation of a pentameric ligand-gated ion channel by a semi-conserved cationic-lipid binding site. J Biol Chem:100899.

Szente L, Puskás I, Vellai T, Lohmann H (2021) Effects of alpha-cyclodextrin on water transport, cell hydration and longevity. Aging 13:1718-1728.

Wang G, Møller-Hansen I, Babaei M, D'Ambrosio V, Christensen HB, Darbani B, Jensen MK, Borodina I (2021) Transportome-wide engineering of Saccharomyces cerevisiae. Metab Eng 64:52-63.

Alijevic O, McHugh D, Rufener L, Mazurov A, Hoeng J, Peitsch M (2020) An electrophysiological characterization of naturally occurring tobacco alkaloids and their action on human alpha4beta2 and alpha7 nicotinic acetylcholine receptors. Phytochemistry 170:112187.

Althaus AL, Ackley MA, Belfort GM, Gee SM, Dai J, Nguyen DP, Kazdoba TM, Modgil A, Davies PA, Moss SJ, Salituro FG, Hoffmann E, Hammond RS, Robichaud AJ, Quirk MC, Doherty JJ (2020) Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABA(A) receptor positive allosteric modulator. Neuropharmacology:108333.

Brams M, Govaerts C, Kambara K, Price KL, Spurny R, Gharpure A, Pardon E, Evans GL, Bertrand D, Lummis SCR, Hibbs RE, Steyaert J, Ulens C (2020) Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site. Elife 9:e51511.

Cieslikiewicz-Bouet M, Naldi M, Bartolini M, Pérez B, Servent D, Jean L, Aráoz R, Renard P-Y (2020) Functional characterization of multifunctional ligands targeting acetylcholinesterase and alpha 7 nicotinic acetylcholine receptor. Biochemical Pharmacology 177:114010.

da Costa Couto A, Price KL, Mesoy S, Capes E, Lummis SCR (2020) The M4 Helix Is Involved in α7 nACh Receptor Function. ACS Chem Neurosci 11:1406-1412.

El Achkar CM, Harrer M, Smith L, Kelly M, Iqbal S, Maljevic S, Niturad CE, Vissers L, Poduri A, Yang E, Lal D, Lerche H, Møller RS, Olson HE (2020) Characterization of the GABRB2-Associated Neurodevelopmental Disorders. Ann Neurol.

Hipp J, Knoflach F, Comley R, Ballard T, Honer M, Trube G, Gasser R, Prinssen EP, Wallace T, Rothfuss A, Henner, Lennon-Chrimes S, Derks M, Squassante L, Nave S, Noeldeke J, Wandel C, Thomas A, Hernandez M-C (2020) Preclinical and Clinical Pharmacology of Basmisanil, a Novel Selective GABAA-α5 Receptor Negative Allosteric Modulator. Authorea.

Malla S, van der Helm E, Darbani B, Wieschalka S, Forster J, Borodina I, Sommer MOA (2020) A Novel Efficient L-Lysine Exporter Identified by Functional Metagenomics. bioRxiv:2020.2004.2030.071142.

Niespodziany I, Ghisdal P, Mullier B, Wood M, Provins L, Kaminski RM, Wolff C (2020) Functional characterization of the antiepileptic drug candidate, padsevonil, on GABAA receptors. Epilepsia.

Özbey NP, Imanikia S, Krueger C, Hardege I, Morud J, Sheng M, Schafer WR, Casanueva MO, Taylor RC (2020) Tyramine Acts Downstream of Neuronal XBP-1s to Coordinate Inter-tissue UPR(ER) Activation and Behavior in C. elegans. Dev Cell.

Rufener L, Kaur K, Sarr A, Aaen SM, Horsberg TE (2020) Nicotinic acetylcholine receptors: Ex-vivo expression of functional, non-hybrid, heteropentameric receptors from a marine arthropod, Lepeophtheirus salmonis. PLoS Pathog 16:e1008715.

Xue W, Mermans C, Papapostolou K-M, Lamprousi M, Christou I-K, Inak E, Douris V, Vontas J, Dermauw W, Van Leeuwen T (2020) Untangling a Gordian knot: the role of a GluCl3 I321T mutation in abamectin resistance in Tetranychus urticae. Pest Management Science n/a.

Zeng SL, Sudlow LC, Berezin MY (2020) Using Xenopus oocytes in neurological disease drug discovery. Expert Opin Drug Discov 15:39-52.

Barth D, Fronius M (2019) Shear force modulates the activity of acid-sensing ion channels at low pH or in the presence of non-proton ligands. Sci Rep 9:6781.

Brams M, Govaerts C, Kambara K, Price KL, Spurny R, Gharpure A, Pardon E, Evans GL, Bertrand D, Lummis SCR, Hibbs RE, Steyaert J, Ulens C (2019) A Functionally Conserved Mechanism of Modulation via a Vestibule Site in Pentameric Ligand-Gated Ion Channels. bioRxiv:770719.

Brissonnet Y, Araoz R, Sousa R, Percevault L, Brument S, Deniaud D, Servent D, Le Questel JY, Lebreton J, Gouin SG (2019) Di- and heptavalent nicotinic analogues to interfere with alpha7 nicotinic acetylcholine receptors. Bioorg Med Chem 27:700-707.

Cameron JM, Maljevic S, Nair U, Aung YH, Cogne B, Bezieau S, Blair E, Isidor B, Zweier C, Reis A, Koenig MK, Maarup T, Sarco D, Afenjar A, Huq A, Kukolich M, Billette de Villemeur T, Nava C, Heron B, Petrou S, Berkovic SF (2019) Encephalopathies with KCNC1 variants: genotype-phenotype-functional correlations. Ann Clin Transl Neurol 6:1263-1272.

Darbani B, Stovicek V, van der Hoek SA, Borodina I (2019) Engineering energetically efficient transport of dicarboxylic acids in yeast Saccharomyces cerevisiae. Proc Natl Acad Sci U S A 116:19415-19420.

Foo CS, Jobichen C, Hassan-Puttaswamy V, Dekan Z, Tae HS, Bertrand D, Adams DJ, Alewood PF, Sivaraman J, Nirthanan S, Kini RM (2019) Fulditoxin, representing a new class of dimeric snake toxins, defines novel pharmacology at nicotinic acetylcholine receptors. Br J Pharmacol.

Gonzalez-Gutierrez JP, Hodar M, Viscarra F, Paillali P, Guerra-Diaz N, Pessoa-Mahana H, Hernandez-Morantes JJ, Perez-Sanchez H, Bermudez I, Reyes-Parada M, Iturriaga-Vasquez P (2019) Minimal Structural Changes Determine Full and Partial Nicotinic Receptor Agonist Activity for Nicotine Analogues. Molecules 24.

Moraga-Nicolás F, Iturriaga-Vásquez P, Mutis A, Hormazábal E, Bermúdez-Díaz I (2019) Galanthamine and other Amaryllidaceae related alkaloids are inhibitors of α7, α4β2 and α3β4 nicotinic acetylcholine receptors. Revista Brasileira de Farmacognosia.

Nielsen BE, Bermudez I, Bouzat C (2019) Flavonoids as positive allosteric modulators of alpha7 nicotinic receptors. Neuropharmacology:107794.

Ornelas-Loredo A, Kany S, Abraham V, Alzahrani Z, Darbar FA, Sridhar A, Ahmed M, Alamar I, Menon A, Zhang M, Chen Y, Hong L, Konda S, Darbar D (2019) Association Between Obesity-Mediated Atrial Fibrillation and Therapy With Sodium Channel Blocker Antiarrhythmic Drugs. JAMA Cardiol.

Otte M, Schweinitz A, Lelle M, Thon S, Enke U, Yuksel S, Schmauder R, Bonus M, Gohlke H, Benndorf K (2019) Novel Fluorescent Cyclic Nucleotide Derivatives to Study CNG and HCN Channel Function. Biophys J.

Park JH, Koko M, Hedrich U, Hermann A, Cremer K, Haberlandt E, Grimmel M, Alhaddad B, Beck-Wödl S, Harrer M, Karall D, Kingelhoefer L, Tzschach A, C. Matthies L, M. Strom T, Ringelstein E, Sturm M, Engels H, Wolff M, Haack T (2019) KCNC1‐related disorders: new de novo variants expand the phenotypic spectrum.

Steidl E, Gleyzes M, Maddalena F, Debanne D, Buisson B (2019) Neuroservice proconvulsive (NS-PC) set: A new platform of electrophysiology-based assays to determine the proconvulsive potential of lead compounds. J Pharmacol Toxicol Methods:106587.

Tiukova IA, Moller-Hansen I, Belew ZM, Darbani B, Boles E, Nour-Eldin HH, Linder T, Nielsen J, Borodina I (2019) Identification and characterisation of two high-affinity glucose transporters from the spoilage yeast Brettanomyces bruxellensis. FEMS Microbiol Lett 366.

van Goethem NP, Paes D, Puzzo D, Fedele E, Rebosio C, Gulisano W, Palmeri A, Wennogle LP, Peng Y, Bertrand D, Prickaerts J (2019) Antagonizing alpha7 nicotinic receptors with methyllycaconitine (MLA) potentiates receptor activity and memory acquisition. Cell Signal 62:109338.

Aguero T, Newman K, King ML (2018) Microinjection of Xenopus Oocytes. Cold Spring Harb Protoc 2018:pdb prot096974.

Amberg W, Lange UEW, Ochse M, Pohlki F, Behl B, Relo AL, Hornberger W, Hoft C, Mezler M, Sydor J, Wang Y, Zhao H, Brewer JT, Dietrich J, Li H, Akritopoulou-Zanze I, Lao Y, Hannick SM, Ku YY, Vasudevan A (2018) Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors. J Med Chem 61:7503-7524.

Danthi SJ, Liang B, Smicker O, Coupland B, Gregory J, Gefteas E, Tietz D, Klodnitsky H, Randall K, Belanger A, Kuntzweiler TA (2018) Identification and Characterization of Inhibitors of a Neutral Amino Acid Transporter, SLC6A19, Using Two Functional Cell-Based Assays. SLAS Discov:2472555218794627.

Henderson SW, Dunlevy JD, Wu Y, Blackmore DH, Walker RR, Edwards EJ, Gilliham M, Walker AR (2018) Functional differences in transport properties of natural HKT1;1 variants influence shoot Na(+) exclusion in grapevine rootstocks. New Phytol 217:1113-1127.

Knoflach F, Hernandez M, Bertrand D (2018) Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission. JoVE:e57842.

Niespodziany I, Mullier B, Andre VM, Ghisdal P, Jnoff E, Moreno-Delgado D, Swinnen D, Sands Z, Wood M, Wolff C (2018) Discovery of a small molecule modulator of the Kv1.1/Kvbeta1 channel complex that reduces neuronal excitability and in vitro epileptiform activity. CNS Neurosci Ther.

Numis AL, Nair U, Datta AN, Sands TT, Oldham MS, Patel A, Li M, Gazina E, Petrou S, Cilio MR (2018) Lack of response to quinidine in KCNT1-related neonatal epilepsy. Epilepsia.

Price KL, Lummis SCR (2018) Characterization of a 5-HT3-ELIC Chimera Revealing the Sites of Action of Modulators. ACS Chem Neurosci 9:1409-1415.

Tang B, Devenish SO, Lummis SCR (2018) Identification of Novel Functionally Important Aromatic Residue Interactions in the Extracellular Domain of the Glycine Receptor. Biochemistry 57:4029-4035.

Tang B, Lummis SCR (2018) Multiple regions in the extracellular domain of the glycine receptor determine receptor activity. J Biol Chem 293:13889-13896.

Tang B, Lummis SCR (2018) The roles of aromatic residues in the glycine receptor transmembrane domain. BMC Neurosci 19:53.

Wang Y, Zhao H, Brewer JT, Li H, Lao Y, Amberg W, Behl B, Akritopoulou-Zanze I, Dietrich J, Lange UEW, Pohlki F, Hoft C, Hornberger W, Djuric SW, Sydor J, Mezler M, Relo AL, Vasudevan A (2018) De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors. J Med Chem.

Zaman SM, Mullen SA, Petrovski S, Maljevic S, Gazina EV, Phillips AM, Jones GD, Hildebrand MS, Damiano J, Auvin S, Lerche H, Weber YG, Berkovic SF, Scheffer IE, Reid CA, Petrou S (2018) Development of a rapid functional assay that predicts GLUT1 disease severity. Neurol Genet 4:e297.

Ast C, Foret J, Oltrogge LM, De Michele R, Kleist TJ, Ho CH, Frommer WB (2017) Ratiometric Matryoshka biosensors from a nested cassette of green- and orange-emitting fluorescent proteins. Nat Commun 8:431.

Becker F, Reid CA, Hallmann K, Tae H-S, Phillips AM, Teodorescu G, Weber YG, Kleefuss-Lie A, Elger C, Perez-Reyes E, Petrou S, Kunz WS, Lerche H, Maljevic S (2017) Functional variants in HCN4 and CACNA1H may contribute to genetic generalized epilepsy. Epilepsia Open 2:334-342.

Bretin S, Louis C, Seguin L, Wagner S, Thomas JY, Challal S, Rogez N, Albinet K, Iop F, Villain N, Bertrand S, Krazem A, Berachochea D, Billiald S, Tordjman C, Cordi A, Bertrand D, Lestage P, Danober L (2017) Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors. PLoS ONE 12:e0184429.

Callahan PM, Bertrand D, Bertrand S, Plagenhoef MR, Terry AV (2017) Tropisetron sensitizes α7 containing nicotinic receptors to low levels of acetylcholine in vitro and improves memory-related task performance in young and aged animals. Neuropharmacology 117:422-433.

Garrood WT, Zimmer CT, Gutbrod O, Lüke B, Williamson MS, Bass C, Nauen R, Emyr Davies TG (2017) Influence of the RDL A301S mutation in the brown planthopper Nilaparvata lugens on the activity of phenylpyrazole insecticides. Pesticide Biochemistry and Physiology.

Giralt A, Gomez-Climent MA, Alcala R, Bretin S, Bertrand D, Maria Delgado-Garcia J, Perez-Navarro E, Alberch J, Gruart A (2017) The AMPA receptor positive allosteric modulator S 47445 rescues in vivo CA3-CA1 long-term potentiation and structural synaptic changes in old mice. Neuropharmacology 123:395-409.

Li M, Maljevic S, Phillips AM, Petrovski S, Hildebrand M, Burgess R, Mount T, Zara F, Striano P, Schubert J, Thiele H, Nürnberg P, Wong M, Weisenberg JL, Thio LL, Lerche H, Scheffer IE, Berkovic SF, Petrou S, Reid CA (2017) Gain-of-function HCN2 variants in genetic epilepsy. Human Mutation:n/a-n/a.

Li M, Milligan CJ, Wang H, Walker A, Churilov L, Lawrence AJ, Reid CA, Hopkins SC, Petrou S (2017) KCTD12 modulation of GABA(B) receptor function. Pharmacol Res Perspect 5:e00319.

Masnada S, Hedrich UBS, Gardella E, Schubert J, Kaiwar C, Klee EW, Lanpher BC, Gavrilova RH, Synofzik M, Bast T, Gorman K, King MD, Allen NM, Conroy J, Ben Zeev B, Tzadok M, Korff C, Dubois F, Ramsey K, Narayanan V, Serratosa JM, Giraldez BG, Helbig I, Marsh E, O’Brien M, Bergqvist CA, Binelli A, Porter B, Zaeyen E, Horovitz DD, Wolff M, Marjanovic D, Caglayan HS, Arslan M, Pena SDJ, Sisodiya SM, Balestrini S, Syrbe S, Veggiotti P, Lemke JR, Møller RS, Lerche H, Rubboli G (2017) Clinical spectrum and genotype–phenotype associations of KCNA2-related encephalopathies. Brain 140:2337-2354.

Mermans C, Dermauw W, Geibel S, Van Leeuwen T (2017) A G326E substitution in the glutamate-gated chloride channel 3 (GluCl3) of the two-spotted spider mite Tetranychus urticae abolishes the agonistic activity of macrocyclic lactones. Pest Manag Sci.

Moller RS, Wuttke TV, Helbig I, Marini C, Johannesen KM, Brilstra EH, Vaher U, Borggraefe I, Talvik I, Talvik T, Kluger G, Francois LL, Lesca G, de Bellescize J, Blichfeldt S, Chatron N, Holert N, Jacobs J, Swinkels M, Betzler C, Syrbe S, Nikanorova M, Myers CT, Larsen LH, Vejzovic S, Pendziwiat M, von Spiczak S, Hopkins S, Dubbs H, Mang Y, Mukhin K, Holthausen H, van Gassen KL, Dahl HA, Tommerup N, Mefford HC, Rubboli G, Guerrini R, Lemke JR, Lerche H, Muhle H, Maljevic S (2017) Mutations in GABRB3: From febrile seizures to epileptic encephalopathies. Neurology 88:483-492.

Mullier B, Wolff C, Sands ZA, Ghisdal P, Muglia P, Kaminski RM, Andre VM (2017) GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors. Neuropharmacology 123:322-331.

Niturad CE, Lev D, Kalscheuer VM, Charzewska A, Schubert J, Lerman-Sagie T, Kroes HY, Oegema R, Traverso M, Specchio N, Lassota M, Chelly J, Bennett-Back O, Carmi N, Koffler-Brill T, Iacomino M, Trivisano M, Capovilla G, Striano P, Nawara M, Rzońca S, Fischer U, Bienek M, Jensen C, Hu H, Thiele H, Altmüller J, Krause R, May P, Becker F, Balling R, Biskup S, Haas SA, Nürnberg P, van Gassen KLI, Lerche H, Zara F, Maljevic S, Leshinsky-Silver E (2017) Rare GABRA3 variants are associated with epileptic seizures, encephalopathy and dysmorphic features. Brain:awx236-awx236.

Price KL, Hirayama Y, Lummis SCR (2017) Subtle Differences among 5-HT3AC, 5-HT3AD, and 5-HT3AE Receptors Are Revealed by Partial Agonists. ACS Chem Neurosci 8:1085-1091.

Principalli MA, Lemel L, Rongier A, Godet AC, Langer K, Revilloud J, Darre L, Domene C, Vivaudou M, Moreau CJ (2017) Functional mapping of the N-terminal arginine cluster and C-terminal acidic residues of Kir6.2 channel fused to a G protein-coupled receptor. Biochim Biophys Acta 1859:2144-2153.

Rufener L, Danelli V, Bertrand D, Sager H (2017) The novel isoxazoline ectoparasiticide lotilaner (Credelio): a non-competitive antagonist specific to invertebrates gamma-aminobutyric acid-gated chloride channels (GABACls). Parasit Vectors 10:530.

Tae HS, Smith KM, Phillips AM, Boyle KA, Li M, Forster IC, Hatch RJ, Richardson R, Hughes DI, Graham BA, Petrou S, Reid CA (2017) Gabapentin Modulates HCN4 Channel Voltage-Dependence. Front Pharmacol 8:554.

Vivaudou M, Todorov Z, Reyes-Mejia GC, Moreau C (2017) Ion Channels as Reporters of Membrane Receptor Function: Automated Analysis in Xenopus Oocytes. In: Membrane Protein Structure and Function Characterization: Methods and Protocols (Lacapere J-J, ed): Springer.

Bürgi JJ, Bertrand S, Marger F, Bertrand D, Reymond J-L (2016) Fluorescent Agonists of the α7 Nicotinic Acetylcholine Receptor Derived from 3-Amino-Quinuclidine. Helvetica Chimica Acta 99:790-804.

Castillo-Gomez E, Oliveira B, Tapken D, Bertrand S, Klein-Schmidt C, Pan H, Zafeiriou P, Steiner J, Jurek B, Trippe R, Pruss H, Zimmermann WH, Bertrand D, Ehrenreich H, Hollmann M (2016) All naturally occurring autoantibodies against the NMDA receptor subunit NR1 have pathogenic potential irrespective of epitope and immunoglobulin class. Mol Psychiatry.

Corbett MA, Bellows ST, Li M, Carroll R, Micallef S, Carvill GL, Myers CT, Howell KB, Maljevic S, Lerche H, Gazina EV, Mefford HC, Bahlo M, Berkovic SF, Petrou S, Scheffer IE, Gecz J (2016) Dominant KCNA2 mutation causes episodic ataxia and pharmacoresponsive epilepsy. Neurology 87:1975-1984.

Diochot S, Alloui A, Rodrigues P, Dauvois M, Friend V, Aissouni Y, Eschalier A, Lingueglia E, Baron A (2016) Analgesic effects of mambalgin peptide inhibitors of acid-sensing ion channels in inflammatory and neuropathic pain. Pain 157:552-559.

Helbig KL, Hedrich UB, Shinde DN, Krey I, Teichmann AC, Hentschel J, Schubert J, Chamberlin AC, Huether R, Lu HM, Alcaraz WA, Tang S, Jungbluth C, Dugan SL, Vainionpaa L, Karle KN, Synofzik M, Schols L, Schule R, Lehesjoki AE, Helbig I, Lerche H, Lemke JR (2016) A recurrent mutation in KCNA2 as a novel cause of hereditary spastic paraplegia and ataxia. Ann Neurol 80.

Johannesen K, Marini C, Pfeffer S, Moller RS, Dorn T, Niturad CE, Gardella E, Weber Y, Sondergard M, Hjalgrim H, Nikanorova M, Becker F, Larsen LH, Dahl HA, Maier O, Mei D, Biskup S, Klein KM, Reif PS, Rosenow F, Elias AF, Hudson C, Helbig KL, Schubert-Bast S, Scordo MR, Craiu D, Djemie T, Hoffman-Zacharska D, Caglayan H, Helbig I, Serratosa J, Striano P, De Jonghe P, Weckhuysen S, Suls A, Muru K, Talvik I, Talvik T, Muhle H, Borggraefe I, Rost I, Guerrini R, Lerche H, Lemke JR, Rubboli G, Maljevic S (2016) Phenotypic spectrum of GABRA1: From generalized epilepsies to severe epileptic encephalopathies. Neurology 87:1140-1151.

Li S, Wang X, Ma QH, Yang WL, Zhang XG, Dawe GS, Xiao ZC (2016) Amyloid precursor protein modulates Nav1.6 sodium channel currents through a Go-coupled JNK pathway. Sci Rep 6:39320.

Maljevic S, Vejzovic S, Bernhard MK, Bertsche A, Weise S, Docker M, Lerche H, Lemke JR, Merkenschlager A, Syrbe S (2016) Novel KCNQ3 Mutation in a Large Family with Benign Familial Neonatal Epilepsy: A Rare Cause of Neonatal Seizures. Mol Syndromol 7:189-196.

Mourier G, Salinas M, Kessler P, Stura EA, Leblanc M, Tepshi L, Besson T, Diochot S, Baron A, Douguet D, Lingueglia E, Servent D (2016) Mambalgin-1 Pain-relieving Peptide, Stepwise Solid-phase Synthesis, Crystal Structure, and Functional Domain for Acid-sensing Ion Channel 1a Inhibition. J Biol Chem 291:2616-2629.

Murenzi E, Toltin AC, Symington SB, Morgan MM, Clark JM (2016) Evaluation of microtransplantation of rat brain neurolemma into Xenopus laevis oocytes as a technique to study the effect of neurotoxicants on endogenous voltage-sensitive ion channels. Neurotoxicology.

Reyes-Mejia GC (2016) Molecular studies of ATP-sensitive potassium channels: Gating, pathology, and optogenetics

Wijckmans E, Nys M, Debaveye S, Brams M, Pardon E, Willegems K, Bertrand D, Steyaert J, Efremov R, Ulens C (2016) Functional and Biochemical Characterization of Alvinella pompejana Cys-Loop Receptor Homologues. PLoS ONE 11:e0151183.

Eggert M, Winterer G, Wanischeck M, Hoda JC, Bertrand D, Steinlein O (2015) The nicotinic acetylcholine receptor alpha 4 subunit contains a functionally relevant SNP Haplotype. BMC Genet 16:46.

Engelhardt K, Schmidt M, Tenbusch M, Dermietzel R (2015) Effects on channel properties and induction of cell death induced by c-terminal truncations of pannexin1 depend on domain length. J Membr Biol 248:285-294.

Li M, Jazayeri D, Corry B, McSweeney KM, Heinzen EL, Goldstein DB, Petrou S (2015) A functional correlate of severity in alternating hemiplegia of childhood. Neurobiol Dis 77:88-93.

Moreau CJ, Niescierowicz K, Caro LN, Revilloud J, Vivaudou M (2015) Ion channel reporter for monitoring the activity of engineered GPCRs. Methods Enzymol 556:425-454.

Muona M, Berkovic SF, Dibbens LM, Oliver KL, Maljevic S, Bayly MA, Joensuu T, Canafoglia L, Franceschetti S, Michelucci R, Markkinen S, Heron SE, Hildebrand MS, Andermann E, Andermann F, Gambardella A, Tinuper P, Licchetta L, Scheffer IE, Criscuolo C, Filla A, Ferlazzo E, Ahmad J, Ahmad A, Baykan B, Said E, Topcu M, Riguzzi P, King MD, Ozkara C, Andrade DM, Engelsen BA, Crespel A, Lindenau M, Lohmann E, Saletti V, Massano J, Privitera M, Espay AJ, Kauffmann B, Duchowny M, Moller RS, Straussberg R, Afawi Z, Ben-Zeev B, Samocha KE, Daly MJ, Petrou S, Lerche H, Palotie A, Lehesjoki AE (2015) A recurrent de novo mutation in KCNC1 causes progressive myoclonus epilepsy. Nat Genet 47:39-46.

Price KL, Lillestol RK, Ulens C, Lummis SC (2015) Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP. ACS Chem Neurosci 6:1151-1157.

Syrbe S, Hedrich UB, Riesch E, Djemie T, Muller S, Moller RS, Maher B, Hernandez-Hernandez L, Synofzik M, Caglayan HS, Arslan M, Serratosa JM, Nothnagel M, May P, Krause R, Loffler H, Detert K, Dorn T, Vogt H, Kramer G, Schols L, Mullis PE, Linnankivi T, Lehesjoki AE, Sterbova K, Craiu DC, Hoffman-Zacharska D, Korff CM, Weber YG, Steinlin M, Gallati S, Bertsche A, Bernhard MK, Merkenschlager A, Kiess W, Gonzalez M, Zuchner S, Palotie A, Suls A, De Jonghe P, Helbig I, Biskup S, Wolff M, Maljevic S, Schule R, Sisodiya SM, Weckhuysen S, Lerche H, Lemke JR (2015) De novo loss- or gain-of-function mutations in KCNA2 cause epileptic encephalopathy. Nat Genet 47:393-399.

Clemencon B, Fine M, Luscher B, Baumann MU, Surbek DV, Abriel H, Hediger MA (2014) Expression, purification, and projection structure by single particle electron microscopy of functional human TRPM4 heterologously expressed in Xenopus laevis oocytes. Protein Expr Purif 95:169-176.

Hassaine G, Deluz C, Grasso L, Wyss R, Tol MB, Hovius R, Graff A, Stahlberg H, Tomizaki T, Desmyter A, Moreau C, Li XD, Poitevin F, Vogel H, Nury H (2014) X-ray structure of the mouse serotonin 5-HT3 receptor. Nature 512:276-281.

Ho CH, Frommer WB (2014) Fluorescent sensors for activity and regulation of the nitrate transceptor CHL1/NRT1.1 and oligopeptide transporters. Elife 3:e01917.

Jones AM, Xuan Y, Xu M, Wang RS, Ho CH, Lalonde S, You CH, Sardi MI, Parsa SA, Smith-Valle E, Su T, Frazer KA, Pilot G, Pratelli R, Grossmann G, Acharya BR, Hu HC, Engineer C, Villiers F, Ju C, Takeda K, Su Z, Dong Q, Assmann SM, Chen J, Kwak JM, Schroeder JI, Albert R, Rhee SY, Frommer WB (2014) Border control--a membrane-linked interactome of Arabidopsis. Science 344:711-716.

Juneja P, Horlacher R, Bertrand D, Krause R, Marger F, Welte W (2014) An Internally Modulated, Thermostable, pH-sensitive Cys Loop Receptor from the Hydrothermal Vent Worm Alvinella pompejana. Journal of Biological Chemistry 289:15130-15140.

Milligan CJ, Li M, Gazina EV, Heron SE, Nair U, Trager C, Reid CA, Venkat A, Younkin DP, Dlugos DJ, Petrovski S, Goldstein DB, Dibbens LM, Scheffer IE, Berkovic SF, Petrou S (2014) KCNT1 gain-of-function in two epilepsy phenotypes is reversed by quinidine. Ann Neurol.

Niescierowicz K, Caro L, Cherezov V, Vivaudou M, Moreau CJ (2014) Functional assay for T4 lysozyme-engineered G protein-coupled receptors with an ion channel reporter. Structure 22:149-155.

De Michele R, Ast C, Loque D, Ho CH, Andrade SL, Lanquar V, Grossmann G, Gehne S, Kumke MU, Frommer WB (2013) Fluorescent sensors reporting the activity of ammonium transceptors in live cells. Elife 2:e00800.

Nieścierowicz K (2013) Developpement de la technologie des Récepteurs Couplés à un Canal Ionique pour des études structure-fonction des Récepteurs Couplés aux Protéines G et du canal Kir6.2. . Laboratoire Canaux dans l'École Doctorale Chimie et Sciences de Vivant DOCTEUR DE L’UNIVERSITÉ DE GRENOBLE

Orhan G, Bock M, Schepers D, Ilina EI, Reichel SN, Loffler H, Jezutkovic N, Weckhuysen S, Mandelstam S, Suls A, Danker T, Guenther E, Scheffer IE, Jonghe PD, Lerche H, Maljevic S (2013) Dominant-negative Effects of KCNQ2 Mutations are Associated with Epileptic Encephalopathy. Ann Neurol.

Spurny R, Billen B, Howard RJ, Brams M, Debaveye S, Price KL, Weston DA, Strelkov SV, Tytgat J, Bertrand S, Bertrand D, Lummis SC, Ulens C (2013) Multisite binding of a general anesthetic to the prokaryotic pentameric Erwinia chrysanthemi ligand-gated ion channel (ELIC). J Biol Chem 288:8355-8364.

Stornaiuolo M, De Kloe GE, Rucktooa P, Fish A, van Elk R, Edink ES, Bertrand D, Smit AB, de Esch IJ, Sixma TK (2013) Assembly of a pi-pi stack of ligands in the binding site of an acetylcholine-binding protein. Nat Commun 4:1875.

Beissner M, Dutertre S, Schemm R, Danker T, Sporning A, Grubmuller H, Nicke A (2012) Efficient Binding of 4/7 alpha-Conotoxins to Nicotinic alpha4beta2 Receptors Is Prevented by Arg185 and Pro195 in the alpha4 Subunit. Mol Pharmacol 82:711-718.

Favreau P, Benoit E, Hocking HG, Carlier L, D' hoedt D, Leipold E, Markgraf R, Schlumberger S, Cordova MA, Gaertner H, Paolini-Bertrand M, Hartley O, Tytgat J, Heinemann SH, Bertrand D, Boelens R, Stocklin R, Molgo J (2012) A novel micro-conopeptide, CnIIIC, exerts potent and preferential inhibition of NaV1.2/1.4 channels and blocks neuronal nicotinic acetylcholine receptors. Br J Pharmacol 166:1654-1668.

Mezler M, Barghorn S, Schoemaker H, Gross G, Nimmrich V (2012) A beta-amyloid oligomer directly modulates P/Q-type calcium currents in Xenopus oocytes. Br J Pharmacol 165:1572-1583.

Murray TA, Bertrand D, Papke RL, George AA, Pantoja R, Srinivasan R, Liu Q, Wu J, Whiteaker P, Lester HA, Lukas RJ (2012) alpha7beta2 nicotinic acetylcholine receptors assemble, function, and are activated primarily via their alpha7-alpha7 interfaces. Mol Pharmacol 81:175-188.

Osipov AV, Rucktooa P, Kasheverov IE, Filkin SY, Starkov VG, Andreeva TV, Sixma TK, Bertrand D, Utkin YN, Tsetlin VI (2012) Dimeric alpha-cobratoxin X-ray structure: localization of intermolecular disulfides and possible mode of binding to nicotinic acetylcholine receptors. J Biol Chem 287:6725-6734.

Prickaerts J, van Goethem NP, Chesworth R, Shapiro G, Boess FG, Methfessel C, Reneerkens OA, Flood DG, Hilt D, Gawryl M, Bertrand S, Bertrand D, Konig G (2012) EVP-6124, a novel and selective alpha7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of alpha7 nicotinic acetylcholine receptors. Neuropharmacology 62:1099-1110.

Utkin YN, Weise C, Kasheverov IE, Andreeva TV, Kryukova EV, Zhmak MN, Starkov VG, Hoang NA, Bertrand D, Ramerstorfer J, Sieghart W, Thompson AJ, Lummis SC, Tsetlin VI (2012) Azemiopsin from Azemiops feae viper venom, a novel polypeptide ligand of nicotinic acetylcholine receptor. J Biol Chem 287:27079-27086.

Baqi Y, Hausmann R, Rosefort C, Rettinger J, Schmalzing G, Muller CE (2011) Discovery of Potent Competitive Antagonists and Positive Modulators of the P2X2 Receptor. J Med Chem.

Bergeron MJ, Boggavarapu R, Meury M, Ucurum Z, Caron L, Isenring P, Hediger MA, Fotiadis D (2011) Frog oocytes to unveil the structure and supramolecular organization of human transport proteins. PLoS ONE 6:e21901.

Kvist T, Hansen KB, Bräuner-Osborne H (2011) The use of Xenopus oocytes in drug screening. Expert Opin Drug Discov 6:141-153.

Thompson AJ, Price KL, Lummis SC (2011) Cysteine modification reveals which subunits form the ligand binding site in human heteromeric 5-HT3AB receptors. J Physiol 589:4243-4257.

Watson GB, Loso MR, Babcock JM, Hasler JM, Letherer TJ, Young CD, Zhu Y, Casida JE, Sparks TC (2011) Novel nicotinic action of the sulfoximine insecticide sulfoxaflor. Insect Biochem Mol Biol.

Zhu Y, Loso MR, Watson GB, Sparks TC, Rogers RB, Huang JX, Gerwick BC, Babcock JM, Kelley D, Hegde VB, Nugent BM, Renga JM, Denholm I, Gorman K, Deboer GJ, Hasler J, Meade T, Thomas JD (2011) Discovery and characterization of sulfoxaflor, a novel insecticide targeting sap-feeding pests. J Agric Food Chem 59:2950-2957.

Bunse S, Schmidt M, Prochnow N, Zoidl G, Dermietzel R (2010) Intracellular cysteine 346 is essentially involved in regulating panx1 channel activity. J Biol Chem 285:38444-38452.

Watson GB, Chouinard SW, Cook KR, Geng C, Gifford JM, Gustafson GD, Hasler JM, Larrinua IM, Letherer TJ, Mitchell JC, Pak WL, Salgado VL, Sparks TC, Stilwell GE (2010) A spinosyn-sensitive Drosophila melanogaster nicotinic acetylcholine receptor identified through chemically induced target site resistance, resistance gene identification, and heterologous expression. Insect Biochem Mol Biol 40:376-384.

Bradaia A, Trube G, Stalder H, Norcross RD, Ozmen L, Wettstein JG, Pinard A, Buchy D, Gassmann M, Hoener MC, Bettler B (2009) The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A 106:20081-20086.

Han N, Vandongen HMA, Vandongen AMJ (2009) Identification of a Novel Class of Allosteric Modulators of the NMDA Receptor. SGH PROCEEDINGS 18.

Zheng T, Clarke AL, Morris MJ, Reid CA, Petrou S, O'Brien TJ (2009) Oxcarbazepine, not its active metabolite, potentiates GABAA activation and aggravates absence seizures. Epilepsia 50:83-87.

Buckingham SD, Pym L, Sattelle DB (2008) Oocytes as an Expression System for Studying Receptor/Channel Targets of Drugs and Pesticides In: Methods in Molecular Biology: Xenopus Protocols - Cell Biology and Signal Transduction (Liu X, ed).

Leisgen C, Kuester M, Methfessel C (2007) The Roboocyte: Automated Electrophysiology Based on Xenopus Oocytes In: Patch Clamp Methods and Protocols (Molnar P, ed): Humana Press.

Goldin AL, ed (2006) Expression of Ion Channels in Xenopus Oocytes. Weinheim: WILEY-VCH Verlag GmbH & Co. KGaA.

Liu L, Zheng T, Morris MJ, Wallengren C, Clarke AL, Reid CA, Petrou S, O'Brien TJ (2006) The mechanism of carbamazepine aggravation of absence seizures. J Pharmacol Exp Ther 319:790-798.

Selenko P, Serber Z, Gadea B, Ruderman J, Wagner G (2006) Quantitative NMR analysis of the protein G B1 domain in Xenopus laevis egg extracts and intact oocytes. Proc Natl Acad Sci U S A 103:11904-11909.

Serber Z, Selenko P, Hansel R, Reckel S, Lohr F, Ferrell JE, Jr., Wagner G, Dotsch V (2006) Investigating macromolecules inside cultured and injected cells by in-cell NMR spectroscopy. Nat Protoc 1:2701-2709.

Shemon AN, Sluyter R, Fernando SL, Clarke AL, Dao-Ung LP, Skarratt KK, Saunders BM, Tan KS, Gu BJ, Fuller SJ, Britton WJ, Petrou S, Wiley JS (2006) A Thr357 to Ser polymorphism in homozygous and compound heterozygous subjects causes absent or reduced P2X7 function and impairs ATP-induced mycobacterial killing by macrophages. J Biol Chem 281:2079-2086.

Zappe S, Fish M, Scott MP, Solgaard O (2006) Automated MEMS-based Drosophila embryo injection system for high-throughput RNAi screens. Lab Chip 6:1012-1019.

Comley J (2005) Automated Patch Clamping. Drug Discovery World:16.

Schnizler K, Saeger B, Pfeffer C, Gerbaulet A, Ebbinghaus-Kintscher U, Methfessel C, Franken EM, Raming K, Wetzel CH, Saras A, Pusch H, Hatt H, Gisselmann G (2005) A novel chloride channel in Drosophila melanogaster is inhibited by protons. J Biol Chem 280:16254-16262.

Pehl U, Leisgen C, Gampe K, Guenther E (2004) Automated higher-throughput compound screening on ion channel targets based on the Xenopus laevis oocyte expression system. Assay Drug Dev Technol 2:515-524.

Schnizler K, Kuster M, Methfessel C, Fejtl M (2003) The roboocyte: automated cDNA/mRNA injection and subsequent TEVC recording on Xenopus oocytes in 96-well microtiter plates. Receptors Channels 9:41-48.

Standhartinger S (2001) Roboter sucht Medikamtenwirkstoffe automatisch. pressetext Austria:2.