Publications

P. Fernandes, D. Pereira, P.B. Watkins, D. Bertrand, Differentiating the Pharmacodynamics and Toxicology of Macrolide and Ketolide Antibiotics, J Med Chem 2019.
S.A. Neale, K. Kambara, T.E. Salt, D. Bertrand, Receptor variants and the development of centrally acting medications, Dialogues Clin Neurosci 21(2) 149-157, 2019.
F. Knoflach, M.C. Hernandez, D. Bertrand, Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission, J Vis Exp (138) 2018.
Bertrand, D and Terry, AV The wonderland of neuronal nicotinic acetylcholine receptors. Biochem Pharmacol 2017.
Callahan, PM, Bertrand, D, Bertrand, S, Plagenhoef, MR and Terry, AV 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 2017;117:422-33.
Rufener, L, Danelli, V, Bertrand, D and Sager, H The novel isoxazoline ectoparasiticide lotilaner (Credelio™): a non-competitive antagonist specific to invertebrates γ-aminobutyric acid-gated chloride channels (GABACls). Parasit Vectors 2017;10:530
Bretin, S, Louis, C, Seguin, L, Wagner, S, Thomas, JY, Challal, S, et al. Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors. PLoS One 2017;12:e0184429.
Knoflach, F, Hernandez, M and Bertrand, D GABA_A receptor-mediated neurotransmission: not so simple after all. Biochemical Pharmacology (2016).
Fernandes, P, Martens, E, Bertrand, D and Pereira, D The Solithromycin Journey – It is all in the Chemistry. Bioorganic & Medicinal Chemistry (2016).
Castillo-Gómez, E, Oliveira, B, Tapken, D, Bertrand, S, Klein-Schmidt, C, Pan, H, et al. All naturally occurring autoantibodies against the NMDA receptor subunit NR1 have pathogenic potential irrespective of epitope and immunoglobulin class. Molecular Psychiatry (2016).
Wijckmans, E, Nys, M, Debaveye, S, Brams, M, Pardon, E, Willegems, K, et al. Functional and Biochemical Characterization of Alvinella pompejana Cys-Loop Receptor Homologues. PLoS One (2016).
Lyukmanova, EN, Shulepko, MA, Shenkarev, ZO, Bychkov, ML, Paramonov, AS, Chugunov, AO, et al. Secreted Isoform of Human Lynx1 (SLURP-2): Spatial Structure and Pharmacology of Interactions with Different Types of Acetylcholine Receptors. Sci Rep (2016).
Bertrand, Daniel, Chih-Hung L Lee, Dorothy Flood, Fabrice Marger, and Diana Donnelly-Roberts. "Therapeutic Potential of α7 Nicotinic Acetylcholine Receptors." Pharmacological reviews (2015).
Eggert, Marlene, Georg Winterer, Mario Wanischeck, Jean-Charles Hoda, Daniel Bertrand, and Ortrud Steinlein. "The Nicotinic Acetylcholine Receptor α4 Subunit Contains a Functionally Relevant SNP Haplotype." BMC genetics (2015).
Spurny, Radovan, Sarah Debaveye, Ana Farinha, Ken Veys, Ann M Vos, Thomas Gossas, John Atack, and others. "Molecular Blueprint of Allosteric Binding Sites in a Homologue of the Agonist-binding Domain of the α7 Nicotinic Acetylcholine Receptor." PNAS (2015).
Stoiljkovic, Milan, Liza Leventhal, Angela Chen, Ting Chen, Rachelle Driscoll, Dorothy Flood, Hilliary Hodgdon, and others. "Concentration-response Relationship of the α7 Nicotinic Acetylcholine Receptor Agonist FRM-17874 Across Multiple in Vitro and in Vivo Assays." BCP (2015).
Terry, Alvin V, Patrick M Callahan, and Daniel Bertrand. "R-(+) and S-(-) Isomers of Cotinine Augment Cholinergic Responses in Vitro and in Vivo." JPET (2015).
Bürgi, J. J., Awale, M., Boss, S. D., Schaer, T., et al. Discovery of Potent Positive Allosteric Modulators of the α3β2 Nicotinic Acetylcholine Receptor by a Chemical Space Walk in ChEMBL. ACS Chem Neurosci (2014).
Juneja, P., Horlacher, R., Bertrand, D., Krause, R., et al. An internally modulated, thermostable, pH sensitive Cys-loop receptor from the hydrothermal vent worm Alvinella pompejana. J Biol Chem (2014).
Rollema, H., Russ, C., Lee, . C., Hurst, . S. & Bertrand, D. Functional Interactions of Varenicline and Nicotine With nAChR Subtypes Implicated in Cardiovascular Control. Nicotine & Tobacco Research (2014).
JA Dani, D Donnelly-Roberts, D Bertrand, Nicotinic acetylcholine receptors as therapeutic targets: Emerging frontiers in basic research and clinical science-Editorial comments., in Biochem Pharmacol
Wallace, T. L. & Bertrand, D. Importance of the nicotinic acetylcholine receptor system in the prefrontal cortex. Biochem Pharmacol 85, 1713-1720 (2013).
Wallace, T. L. & Bertrand, D. Alpha7 neuronal nicotinic receptors as a drug target in schizophrenia. Expert Opin Ther Targets 17, 139-155 (2013).
Spurny, R., Billen, B., Howard, R. J., Brams, M., et al. Multisite binding of a general anesthetic to the prokaryotic pentameric Erwinia chrysanthemi ligand-gated ion channel (ELIC). J Biol Chem 288, 8355-8364 (2013).
Lyukmanova, E. N., Shulepko, M. A., Buldakova, S. L., Kasheverov, I. E., et al. Water-soluble LYNX1 residues important for interaction with muscle-type and/or neuronal nicotinic receptors. J Biol Chem 288, 15888-15899 (2013).
Stornaiuolo, M., De Kloe, G. E., Rucktooa, P., Fish, A., et al. Assembly of a π-π stack of ligands in the binding site of an acetylcholine-binding protein. Nat Commun 4, 1875 (2013).
Prestori, F., Bonardi, C., Mapelli, L., Lombardo, P., et al. Gating of long-term potentiation by nicotinic acetylcholine receptors at the cerebellum input stage. PLoS One 8, e64828 (2013).
Favreau, P., Benoit, E., Hocking, H. G., Carlier, L., et al. Pharmacological characterization of a novel μ-conopeptide, CnIIIC, indicates potent and preferential inhibition of sodium channel subtypes (Na(V) 1.2/1.4) and reveals unusual activity on neuronal nicotinic acetylcholine receptors. Br J Pharmacol 166, 1654-1668 (2012).
Utkin, Y. N., Weise, C., Kasheverov, I. E., Andreeva, T. V., et al. Azemiopsin from Azemiops feae viper venom, a novel polypeptide ligand of nicotinic acetylcholine receptor. J Biol Chem (2012).
Osipov, A. V., Rucktooa, P., Kasheverov, I. E., Filkin, S. Y., et al. Dimeric α-cobratoxin X-ray structure: localization of intermolecular disulfides and possible mode of binding to nicotinic acetylcholine receptors. J Biol Chem 287, 6725-6734 (2012).
Bréthous, L., Garcia-Delgado, N., Schwartz, J., Bertrand, S., et al. Synthesis and Nicotinic Receptor Activity of Chemical Space Analogues of N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-Diazabicyclo[3.2.2]nonane-4-carboxylic Acid 4-Bromophenyl Ester (SSR180711). J Med Chem (2012).
Hurst, R., Rollema, H. & Bertrand, D. Nicotinic acetylcholine receptors: From basic science to therapeutics. Pharmacol Ther (2012).
Billen, B., Spurny, R., Brams, M., van Elk, R., et al. Molecular actions of smoking cessation drugs at α4β2 nicotinic receptors defined in crystal structures of a homologous binding protein. Proc Natl Acad Sci U S A (2012).
Steinlein, O. K., Hoda, J. C., Bertrand, S. & Bertrand, D. Mutations in familial nocturnal frontal lobe epilepsy might be associated with distinct neurological phenotypes. Seizure 21, 118-123 (2012).
Reymond, J. L., van Deursen, R. & Bertrand, D. What we have learned from crystal structures of proteins to receptor function. Biochem Pharmacol (2011).
Donnelly-Roberts, D., Bertrand, D. & Gopalakrishnan, M. Nicotinic acetylcholine receptors as therapeutic targets: Emerging frontiers in basic research and clinical science-Editorial Comments. Biochem Pharmacol 82, 797 (2011).
Araud, T., Graw, S., Berger, R., Lee, M., et al. The chimeric gene CHRFAM7A, a partial duplication of the CHRNA7 gene, is a dominant negative regulator of α7*nAChR function. Biochem Pharmacol 82, 904-914 (2011).
Wallace, C., Porter, P., Neveu, E. & Bertrand, D. Effects of RG3487 at the a7b2 nicotinic acetylcholine receptor expressed in Xenopus oocytes. Biochemical Pharmacology 82, 1026 (2011).
Akdemir, A., Rucktooa, P., Jongejan, A., Elk, R., et al. Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors. Bioorg Med Chem 19, 6107-6119 (2011).
Czarnetzki, C., Schiffer, E., Lysakowski, C., Haller, G., et al. Transcutaneous nicotine does not prevent postoperative nausea and vomiting: a randomized controlled trial. Br J Clin Pharmacol 71, 383-390 (2011).
Pucci, L., Grazioso, G., Dallanoce, C., Rizzi, L., et al. Engineering of {alpha}-conotoxin MII-derived peptides with increased selectivity for native {alpha}6{beta}2* nicotinic acetylcholine receptors. FASEB J (2011).
Lyukmanova, E. N., Shenkarev, Z. O., Shulepko, M. A., Mineev, K. S., et al. NMR STRUCTURE AND ACTION ON NICOTINIC ACETYLCHOLINE RECEPTORS OF WATER-SOLUBLE DOMAIN OF HUMAN LYNX1. J Biol Chem (2011).
Blum, L. C., van Deursen, R., Bertrand, S., Mayer, M., et al. Discovery of α7-nicotinic receptor ligands by virtual screening of the chemical universe database GDB-13. J Chem Inf Model 51, 3105-3112 (2011).
Murray, T. A., Bertrand, D., Papke, R. L., George, A. A., et al. α7β2 nAChRs Assemble and Function, and are Activated Primarily Via their α7-α7 Interfaces. Mol Pharmacol 81, 175-188 (2011).
Prickaerts, J., van Goethem, N. P., Chesworth, R., Shapiro, G., et al. EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. Neuropharmacology 62, 1099-1110 (2011).
Rollema, H., Bertrand, D. & Hurst, R. in SpringerReference (Springer-Verlag, Berlin/Heidelberg, 2011).
Garcia-Delgado, N., Bertrand, S., Nguyen, K. T., van Deursen, R., et al. Exploring a7-Nicotinic Receptor Ligand Diversity by Scaffold Enumeration from the Chemical Universe Database GDB. ACS Medicinal Chemistry Letters 1, 422-426 (2010).
Bertrand, D., Bertrand, S., Neveu, E. & Fernandes, P. Molecular characterization of off-target activities of telithromycin: a potential role for nicotinic acetylcholine receptors. Antimicrob Agents Chemother 54, 5399-5402 (2010).
Araud, T., Wonnacott, S. & Bertrand, D. Associated proteins: The universal toolbox controlling ligand gated ion channel function. Biochem Pharmacol 80, 160-169 (2010).
Mony, L., Triballeau, N., Paoletti, P., Acher, F. C. & Bertrand, H. O. Identification of a novel NR2B-selective NMDA receptor antagonist using a virtual screening approach. Bioorg Med Chem Lett 20, 5552-5558 (2010).
Rollema, H., Shrikhande, A., Ward, K. M., Tingley Iii, F. D., et al. Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence. Br J Pharmacol (2010).
Bertrand, D. Neurocircuitry of the nicotinic cholinergic system. Dialogues Clin Neurosci 12, 463-470 (2010).
Roy, A., Zhou, X., Chong, M. Z., D'hoedt, D., et al. Structural and Functional Characterization of a Novel Homodimeric Three-finger Neurotoxin from the Venom of Ophiophagus hannah (King Cobra). J Biol Chem 285, 8302-8315 (2010).
Nury, H., Bocquet, N., Le Poupon, C., Raynal, B., et al. Crystal structure of the extracellular domain of a bacterial ligand-gated ion channel. J Mol Biol 395, 1114-1127 (2010).
Wallace, T. L., Callahan, P. M., Tehim, A., Bertrand, D., et al. RG3487, a Novel Nicotinic Alpha7 Receptor Partial Agonist, Improves Cognition and Sensorimotor Gating in Rodents. J Pharmacol Exp Ther 336, 242-253 (2010).
Wallace, T. L., Chiu, G., Dao, H., Santarelli, L., et al. Modulation of Cholinergic Tone Impacts the Efficacy of RG3487 / MEM3454, A Novel, Nicotinic Alpha 7 Receptor Agonist. Society for Neuroscience Meeting 236.1 (2010).