BENZON SYMPOSIUM No. 47 Molecular Pharmacology of Ion Channels

August 13-17, 2000 – Copenhagen, Denmark

Organizing committee: Jan Egebjerg, Søren-P. Olesen, Povl Krogsgaard-Larsen

Synopsis: Activation of ion channels is essential for most cellular responses of both excitable and non-excitable cells. The primary structure of the protein building blocks of the majority of these ion channels has been determined, and different approaches have revealed detailed information on the mechanism of channel activation and regulation. In addition, structural elements defining the functional domain of the channel proteins have been identified and shown to exhibit structural homology between evolutionary distantly related channel proteins.

Ion channels are targets for a large number of commonly used therapeutic agents. Many drugs act specifically on molecular subtypes of ion channels. The structural basis underlying the selectivity and the specific mode of action of a number of drugs have provided invaluable information on the molecular mechanism for ion channel activation and disclosed potential new targets for novel drugs. Moreover, genetic methods have provided the means to alter the pharmacological profile of ion channels and to study the animal behavioral effects of drugs.

The aim of the symposium is to discuss the molecular mechanisms of ion channel activation and regulation with emphasis on molecular pharmacological approaches combined with “state of the art” molecular biological techniques.

Invited speakers: Stephen Heinemann, William N. Zagotta, Rolf Sprengel, Hey-Kyoung Lee, Mark Mayer, David Clapham, Frances Ashcroft, Thomas J. Jentsch, Eric Gouaux, Richard W. Tsien, Arthur Karlin, Michel Lazdunski, Heinrich Betz, David Julius, Bjarke Ebert, John A. Dani, William A. Catterall, Senyon Choe, Hanns Möhler, Michael Cahalan, Chris Miller, R. Alan North, John Adelman, Juan Lerma

Scientific Programme:

Session I: GLUTAMATE RECEPTORS I
Stephen Heinemann: Kainate Receptor-Deficient Mice
Rolf Sprengel: Importance of AMPA Receptors in Synaptic Plasticity
Hey-Kyoung Lee: Regulation of Glutamate Receptor Function and Synaptic Plasticity
Juan Lerma: Kainate Receptors: New Functions, New Mechanisms

Session II: GLUTAMATE RECEPTORS II
Eric Gouaux: Action of Agonists and Antagonists on the GluR2 Ligand Binding Core Defined by X-ray Crystallography
Jan Egebjerg: Molecular Pharmacology of the Recombinant Glutamate Receptors
Mark Mayer: Block of Glutamate Receptor Channels by Polyamines

Poster session (Posters Nos. 1-21 incl.)

Session III: NUCLEOTIDE-GATED AND INHIBITORY RECEPTORS
R. Alan North: Structure and Function in P2X Receptors
Heinrich Betz: Inhibitory and Excitatory Glycine Receptors: Structures, Functions and Synaptic Localization
Hanns Möhler: GABAA Receptor Functions in vivo Revealed by Targeted Point Mutations
Bjarke Ebert: GABAA Receptors: Determinants of Agonist Activity

Session IV: NICOTINIC ACETYLCHOLINE RECEPTORS
Selected oral presentations:
Michael Hollmann: Functional Concatemeric Glutamate Receptors Suggest a Tetrameric Receptor Complex Stoichiometry (Poster NO. 6)
Bodo Laube: Molecular Determinants of Agonist Discrimination in the NR2B Subunit of the Excitatory NMDA Receptor (Poster NO. 15)
Roger L. Papke: Kinetic Analysis of alpha7 nAChR Fast Desensitization In Acutely Dissociated Hypothalamic Neurons: Implications for Therapeutics (Poster NO. 30)
Bruce Cohen: Probing Potassium Channel Dynamics With a Unique Intrinsic Fluorescence (Poster NO. 33)
John A. Dani: Nicotinic Cholinergic Mechanisms in the Central Nervous System
Arthur Karlin: Gating and Electrostatics in the Acetylcholine Receptor Channel

Poster session (Posters Nos. 22-37 incl.)

Session V: POTASSIUM CHANNELS I
David Clapham: Gβγ Regulated Ion Channels In Heart and Brain
Senyon Choe: Tetrameric Assembly of Voltage-gated K+ Channels
Chris Miller: Structure-driven Investigations to Voltage-gated K+ Channels
Frances Ashcroft: Gating of the KATP Channel and Its Modulation by Mg-Nucleotides

Session VI: POTASSIUM CHANNELS II
John Adelman: Structure, Function, and Physiology of Small and Conductance Calcium-activated Potassium Channels
Søren-Peter Olesen: Molecular Pharmacology of Calcium-activated K+ Channels
Michel Lazdunski: 2P-Domain K+ Channels: Structure, Physiological Functions, Parmacology and Therapeutic Implications

Poster session (Posters Nos. 38-59 incl.)

Session VII: CA-PERMEABLE CHANNELS
Michael Cahalan: Cracking the Puzzles of CRAC, Ca2+ Release-activated Ca2+ Channels in Human T Lymphocytes
William N. Zagotta: Molecular Mechanisms of Gating in Cyclic Nucleotide-gated Channels
David Julius: Ion Channels in the Pain Pathway
Richard W. Tsien: New Perspectives on Structure and Function of Voltage-gated Calcium Channels

Session VIII: CHLORIDE AND SODIUM CHANNELS

Selected oral presentations:
Andy Randall: Electrophysiological Analysis of the Vanilloid Receptor (VR1): Studies of Recombinant Receptors and Knockout Mice (Poster NO. 66)
Bernard Attali: Modulation of the Cardiac IKS Channel Gating: the Same IsK Residues Slow Activation and Prevent Channel Inactivation (Poster NO. 38) v Kamilla A. Pedersen: A Novel Toxin-blocker of the ERG1 Channel (Poster NO. 51)
Carlo Brugnara: Oral Administration of Novel Blocker of Erythrocyte Cl-Conductance (NS3623) Reduces Sickle Cell Dehydration and Sickling In Transgenic Sickle (SAD) Mice (Poster NO. 69)
Thomas J. Jentsch: Diseases Due to Chloride and Potassium Channel Mutations
William A. Catterall: Structure, Function, and Molecular Pharmacology Voltage-gated Sodium Channels

Poster session (Posters Nos. 60-78 incl.)

Abstracts (pdf)